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Adrenergic Beta Receptor

Adrenergic receptors are a class of -coupled receptors that are targets of the , especially and epinephrine. Many cells possess these receptors, and the binding of a to the receptor will generally stimulate the sympathetic nervous system. The sympathetic nervous system is responsible for the fight-or-flight response, which includes widening the pupils of the eye, mobilizing energy, and diverting blood flow from non-essential organs to skeletal muscle. There are two main groups of adrenergic receptors, α and β, with several subtypes. α receptors have the subtypes α1 and α2. β receptors have the subtypes β1, β2 and β3. All three are linked to Gs proteins, which in turn are linked to adenylate cyclase. binding thus causes a rise in the intracellular concentration of the second messenger cAMP. Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates some of the intracellular events following hormone binding.

www.MedChemExpress.com 1 , Antagonists, Inhibitors, Activators & Modulators

(+)- (4E)-SUN9221 ((R)-Penbutolol; (+)-Isopenbutolol) Cat. No.: HY-116790A Cat. No.: HY-U00367

(+)-Penbutolol is a β-adrenoceptor antagonist, (4E)-SUN9221 is a potent antagonist of

with an IC50 of 0.74 μM. (+)-Penbutolol is an α1-adrenergic receptor and 5-HT2 receptor, with optical isomer of l-penbutolol with Na+ antihypertensive and anti-platelet aggregation channel-blocking action. activities.

Purity: >95.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

(R)-(+)- (R)- Cat. No.: HY-B2111 ((R)-BM 14190) Cat. No.: HY-B0006C

(R)-(+)-Atenolol is the less active enantiomer of (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of the (R,S)-atenolol. (R,S)-atenolol is a Carvedilol, is a non-selective β/α-1 blocker. β-adrenergic . (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).

Purity: >99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 1 mg, 5 mg

(R)- (Rac)- hydrochloride Cat. No.: HY-B0371B Cat. No.: HY-15394

(R)-Terazosin is an active R-enantiomer of (Rac)-Rotigotine hydrochloride is a racemate of Terazosin. (R)-Terazosin is a potent Rotigotine.

α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.

Purity: 99.77% Purity: 97.76% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

(RS)-Butyryltimolol (S)-Carvedilol Cat. No.: HY-102032A ((S)-BM 14190) Cat. No.: HY-B0006B

(RS)-Butyryltimolol is the racemate of (S)-Carvedilol, the S-enantiomer of Carvedilol, is Butyryltimolol. Butyryltimolol, an effective a non-selective β/α-1 blocker. (S)-Carvedilol prodrug of , improves the corneal exerts protection against the vascular or cardiac penetration of Timolol. Butyryltimolol is a toxicity of Doxorubicin (DOX). β-adrenergic blocker.

Purity: >98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

(S)-Terazosin (S)-Timolol Maleate Cat. No.: HY-B0371D (L-714,465 Maleate; MK 950) Cat. No.: HY-17380

(S)-Terazosin is an active S-enantiomer of (S)-Timolol Maleate (L-714,465 Maleate) is a Terazosin. (S)-Terazosin is a potent and non-cardioselective hydrophilic β-adrenoceptor

high-affinity α-adrenoceptor antagonist with Ki blocker. (S)-Timolol Maleate is widely used as values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, standard for intraocular pressure α1b and α1d-adrenoceptor, respectively. (glaucoma) by preventing the production of aqueous humor. Purity: 99.77% Purity: 99.85% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 100 mg, 200 mg

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(±)-Befunolol (±)-Bisoprolol hemifumarate Cat. No.: HY-101752 ( hemifumarate salt) Cat. No.: HY-B0076

(±)- is a β-adrenoceptor blocking agent. (±)-Bisoprolol (hemifumarate) is a selective type β1 adrenergic receptor blocker. Target: Adrenergic Receptor Approved: July 31, 1992 Bisoprolol, on beta 1-adrenoceptor induced autoimmune myocardial damage.

Purity: >98% Purity: 99.65% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg

2',5'-Dideoxyadenosine 4-Hydroxypropranolol D7 hydrochloride Cat. No.: HY-135878 ((±)-4-hydroxy D7 hydrochloride) Cat. No.: HY-100634S

2',5'-Dideoxyadenosine is a potent and 4-Hydroxypropranolol D7 hydrochloride non-competitive inhibitor via ((±)-4-hydroxy Propranolol D7 hydrochloride) is a binding the P-site with an IC50 of 3 µM . deuterium labeled 4-Hydroxypropranolol 2',5'-Dideoxyadenosine is a nucleoside analog and hydrochloride. exerts a potent antiadrenergic action in heart.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg, 250 mg Size: 1 mg, 5 mg

4-Hydroxypropranolol hydrochloride 5-HT2 antagonist 1 ((±)-4-hydroxy Propranolol hydrochloride) Cat. No.: HY-100634 Cat. No.: HY-U00365

4-Hydroxypropranolol hydrochlorid is an active 5-HT2 antagonist 1 is a potent antagonist of metabolite of Propranolol. 4-Hydroxypropranolol 5-HT2 receptor, with weak α1 adrenoceptor hydrochlorid is of comparable potency to blocking activity. Propranolol.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Aaptamine D7 Cat. No.: HY-N4225 Cat. No.: HY-17497S

Aaptamine, a spongean isolated from a sea Acebutolol D7 is a deuterium labeled Acebutolol. sponge Aaptos aaptos, is a competitive antagonist Acebutolol is a selective β1 adrenergic receptor of α-adrenoceptor and activates the p21 promoter antagonist used in the treatment of , in a p53-independent manner. angina pectoris and cardiac arrhythmias.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Acebutolol hydrochloride ACTH (1-14) Cat. No.: HY-17497A (Adrenocorticotropic Hormone Fragment 1-14) Cat. No.: HY-P1582

Acebutolol hydrochloride is a β1 adrenergic ACTH (1-14) is a fragment of adrenocorticotrophin, receptor (β1AR) antagonist. Acebutolol which regulates cortisol and androgen production. hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

Purity: 99.95% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 5 g, 10 g Size: 1 mg, 5 mg

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ACTH (1-14) (TFA) ADRA1D receptor agonist 1 (Adrenocorticotropic Hormone Fragment 1-14 TFA) Cat. No.: HY-P1582A Cat. No.: HY-135270

ACTH (1-14) (TFA) is a fragment of ADRA1D receptor agonist 1 (compound (R)-9S) is a

adrenocorticotrophin, which regulates cortisol and potent, selective and orally active α1D

androgen production. adrenoceptor antagonist, with a Ki of 1.6 nM.

Purity: 98.55% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg

AGN 192836 Cat. No.: HY-100300 (Raubasine) Cat. No.: HY-N1919

AGN 192836 is a potent and selective α2 adrenergic Ajmalicine (Raubasine) is found in herbs of

agonist with EC50s of 8.7, 41 and 6.6 nM for Catharanthus roseus, is an antihypertensive α2A, α2B and α2C receptor, respectively. used in the treatment of high , decreases peripheral resistance and blood pressure.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Alfuzosin hydrochloride (SL 77499) Cat. No.: HY-B0192 (SL 77499-10) Cat. No.: HY-B0192A

Alfuzosin is an α1 adrenergic receptor antagonist Alfuzosin hydrochloride is an α1 adrenergic used to treat benign prostatic hyperplasia (BPH). receptor antagonist used to treat benign prostatic hyperplasia (BPH).

Purity: 99.81% Purity: 98.73% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

Amezinium methylsulfate hydrochloride (Amezinium metilsulfate; Lu-1631) Cat. No.: HY-A0275 (SR 58611A) Cat. No.: HY-103207

Amezinium metilsulfate has multiple mechanisms, Amibegron hydrochloride is a selective

including stimulation of alpha and beta-1 β3-adrenoceptor agonist, with an EC50 of 3.5 nM receptors and inhibition ofnoradrenaline and for β-adrenoceptor in rat colon; Amibegron uptake. hydrochloride has and activity.

Purity: 99.51% Purity: >99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg, 1 g Size: 5 mg

Amitraz (BTS-27419) Cat. No.: HY-B1111 Cat. No.: HY-100141

Amitraz is a non-systemic acaricide and Ancarolol is a beta-adrenergic blocking agent. insecticide, with alpha- activity, interaction with receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.

Purity: >98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

AR-08 Cat. No.: HY-U00371 Cat. No.: HY-16056

AR-​08 is an agonist of α2-adrenergic receptor, Arbutamine is a short-acting synthetic potent used for the treatment of attention deficit nonselective β-adrenoceptor agonist that hyperactivety disorder (ADHD). increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine is a catecholamine for a pharmacological cardiac stress agen. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Arotinolol Cat. No.: HY-122537A (Org 5222) Cat. No.: HY-10121

Arotinolol is a nonselective α/β-adrenergic Asenapine(Org 5222) inhibits adrenergic receptor receptor blocker and a vasodilating β-blocker. (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and Arotinolol also shows potency for inhibiting the also inhibits 5-HT receptor (1A, 1B, 2A, 2B, , binding of the radioligand 125I-ICYP to 5A, 6, 7) with Ki of 0.03-4.0 nM.

5HT1B- receptor sites.

Purity: 98.18% Purity: 98.81% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Atenolol ((RS)-Atenolol) Cat. No.: HY-17498 (MPV 1248) Cat. No.: HY-12380A

Atenolol is a selective β1 receptor antagonist. Atipamezole is a synthetic α2-adrenoceptor

Target: Adrenergic Receptor Atenolol is a antagonist with a Ki of 1.6 nM. cardioselective beta-adrenergic blocker possessing properties and potency similar to propranolol, but without a negative inotropic effect [1, 2].

Purity: 99.61% Purity: 99.48% Clinical Data: Launched Clinical Data: Phase 1 Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 10 mM × 1 mL, 10 mg, 50 mg

Atipamezole hydrochloride (MPV-1248 hydrochloride) Cat. No.: HY-12380 ((±)-Bambuterol; KWD-2183) Cat. No.: HY-17501

Atipamezole hydrochloride is a synthetic Bambuterol ((±)-Bambuterol; KWD-2183) is a long

α2-adrenoceptor antagonist with a Ki of 1.6 nM. acting beta-adrenoceptor agonist (LABA) used in the treatment of ; it also is a prodrug of .

Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 1 mg, 5 mg

Bambuterol hydrochloride Batefenterol ((±)-Bambuterol hydrochloride; KWD-2183 hydrochloride) Cat. No.: HY-17501A (GSK961081; TD-5959) Cat. No.: HY-12980

Bambuterol hydrochloride ((±)-Bambuterol Batefenterol (GSK961081;TD-5959) is a novel hydrochloride; KWD-2183 hydrochloride) is a long muscarinic receptor antagonist and acting beta-adrenoceptor agonist (LABA) used in β2-adrenoceptor agonist; displays high affinity the treatment of asthma; it also is a prodrug of for hM2, hM3 muscarinic and hβ2-adrenoceptor with terbutaline. Ki values of 1.4, 1.3 and 3.7 nM, respectively.

Purity: 99.57% Purity: 98.17% Clinical Data: Launched Clinical Data: Phase 2 Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

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Benzquinamide (P2647; BZQ; Benzoquinamide) Cat. No.: HY-U00244 Cat. No.: HY-B0381

Benzquinamide (P2647) is an antiemetic which can Betaxolol is a selective beta1 adrenergic receptor

bind to the α2A, α2B, and α2C adrenergic blocker used in the treatment of hypertension and

receptors (α2-AR) with Ki values of 1,365, 691, glaucoma. Target: Beta1 Adrenergic Receptor and 545 nM, respectively. Betaxolol is a cardioselective beta-adrenergic receptor blocking agent. Betaxolol (5 mg/kg via i.p. Purity: >98% Purity: 96.95% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Betaxolol hydrochloride hydrochloride (SL75212) Cat. No.: HY-B0381A Cat. No.: HY-121186

Betaxolol Hydrochloride is a selective beta1 Bevantolol hydrochloride is a selective β1 and

adrenergic receptor blocker used in the treatment α1-adrenergic receptor antagonist with pKi values of hypertension and glaucoma. Target: Beta1 of 7.83, 6.9 in rat cerebral cortex, respectively. Adrenergic Receptor Betaxolol hydrochloride is a Bevantolol hydrochloride is a potent Ca2+ cardioselective beta-adrenergic receptor blocking antagonist. agent. Purity: 98.94% Purity: >98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 25 mg, 50 mg, 100 mg

BI-167107 Bometolol Hydrochloride Cat. No.: HY-121251 Cat. No.: HY-U00386

BI-167107 is a high affinity, full agonist that Bometolol Hydrochloride is a beta-adrenergic binds to the β2 adrenergic receptor (β2AR) with a blocking agent, used for the research of

dissociation constant Kd of 84 pM. cardiovascular disease.

Purity: 99.81% Purity: >98% Clinical Data: Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Brimonidine tartrate (UK 14304; AGN190342) Cat. No.: HY-B0659 (UK 14304 tartrate; AGN190342 tartrate) Cat. No.: HY-B0659A

Brimonidine (UK 14304) is a full α2-adrenergic Brimonidine tartrate (UK 14304 tartrate) is a full receptor (α2-AR) agonist. α2-adrenergic receptor (α2-AR) agonist.

Purity: 99.65% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

BRL 37344 sodium Brombuterol D9 (BRL 37344A) Cat. No.: HY-101325 (Bromobuterol D9) Cat. No.: HY-131104S

BRL 37344 sodium (BRL 37344A) is a specific Brombuterol D9 (Bromobuterol D9) is a deuterium β3-adrenergic receptor agonist. BRL 37344 sodium labeled Brombuterol. Brombuterol is a β-adrenergic treatment significantly lowers the body weight of receptor agonist. obese mice.

Purity: >99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg

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Brombuterol D9 hydrochloride Brombuterol hydrochloride (Bromobuterol D9 hydrochloride) Cat. No.: HY-131104AS (Bromobuterol hydrochloride) Cat. No.: HY-131145

Brombuterol D9 hydrochloride (Bromobuterol D9 Brombuterol hydrochloride (Bromobuterol hydrochloride) is a deuterium labeled Brombuterol hydrochloride) is a β-adrenergic receptor agonist. hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Bucindolol Carbazochrome sodium sulfonate Cat. No.: HY-103214 (AC-17) Cat. No.: HY-B0491A

Bucindolol is a β1-adrenergic receptor blocker, Carbazochrome (sodium sulfonate) (AC-17) is an with intrinsic sympathomimetic activity, used in antihemorrhagic agent. the research of .

Purity: >99.0% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg

Carteolol hydrochloride Carvedilol (OPC-1085 hydrochloride) Cat. No.: HY-17495A (BM 14190) Cat. No.: HY-B0006

Carteolol hydrochloride (OPC-1085 hydrochloride) Carvedilol (BM 14190) is a non-selective β/α-1 is a non-selective used to treat blocker. Carvedilol inhibits lipid peroxidation in glaucoma. a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Purity: 99.96% Purity: 99.93% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

Carvedilol phosphate hemihydrate Centanafadine (BM 14190 phosphate hemihydrate) Cat. No.: HY-B0006A (EB-1020) Cat. No.: HY-16736

Carvedilol phosphate hemihydrate (BM 14190 Centanafadine is dual norepinephrine (NE)/ phosphate hemihydrate) is a non-selective β/α-1 (DA) transporter inhibitor, also inhibits blocker. Carvedilol phosphate hemihydrate inhibits transporter, with IC50s of 6 nM, 38 nM lipid peroxidation with an IC50 of 5 μM. and 83 nM for human NE, DA and serotonin transporter , respectively.

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Centanafadine hydrochloride CGP 20712 A (EB-1020 hydrochloride) Cat. No.: HY-16736A (CGP 20712 mesylate) Cat. No.: HY-101355B

Centanafadine (hydrochloride) is dual CGP 20712 A (CGP 20712 mesylate) is a highly norepinephrine (NE)/dopamine (DA) transporter selective β1-adrenoceptor inhibitor, also inhibits serotonin transporter, antagonist with an IC50 of 0.7 nM. CGP 20712 A with IC50s of 6 nM, 38 nM and 83 nM for human NE, exhibits ~10,000-fold selectivity over DA and serotonin transporter , respectively. β2-adrenoceptors.

Purity: 99.93% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

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Cicloprolol hydrochloride -D7 Cat. No.: HY-U00066 Cat. No.: HY-100935S

Cicloprolol is a partial β 1-adrenoceptor Cimaterol-D7 is the deuterium labeled Cimaterol. agonist . Cimaterol is a potent agonist of β-adrenergic

receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Cimbuterol-D9 CL 316243 Cat. No.: HY-131105S Cat. No.: HY-116771A

Cimbuterol-D9 is the deuterium labeled Cimbuterol. CL316243 is a highly potent selective

Cimbuterol is aβ-adrenergic agonist. β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg

Clenproperol Clenproperol-D7 Cat. No.: HY-100699 Cat. No.: HY-100699S

Clenproperol is a β2-adrenergic agonist. Clenproperol-D7 is the deuterium labeled Clenproperol. Clenproperol is a β2-adrenergic agonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Clonidine hydrochloride Cat. No.: HY-12721 Cat. No.: HY-B0409A

Clonidine is an alpha 2-adrenergic agonist which is Clonidine hydrochloride is an agonist of used extensively in anesthesia research. α2-adrenoceptor and potent antihypertensive agent.

Purity: 98.79% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

Clorprenaline D7 Clorprenaline hydrochloride Cat. No.: HY-131106S Cat. No.: HY-B1347

Clorprenaline D7 is a deuterium labeled Clorprenaline hydrochloride is a β2-adrenergic Clorprenaline. Clorprenaline is a β2-adrenergic receptor agonist that is implicated in bronchial receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for expansion. Clorprenaline has the potential for asthma research. asthma research.

Purity: >98% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg

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D2343 Dabuzalgron Cat. No.: HY-U00206 (Ro 115-1240) Cat. No.: HY-117071

D2343 is a β2-adrenoceptor agonist and also is an Dabuzalgron (Ro 115-1240) is an orally active and α1- adrenoceptor inhibitor. selective α-1A adrenergic receptor agonist for the treatment of . Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function. Purity: >98% Purity: 98.72% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

Dapiprazole hydrochloride Deriglidole Cat. No.: HY-A0142A (SL 86-0715) Cat. No.: HY-101683

Dapiprazole hydrochloride is a potent α-adrenergic Deriglidole is a peripheral adrenoceptor blocking drug, which is used to reverse mydriasis antagonist with a high affinity for after eye examination. α2-adrenoceptors.

Purity: 99.97% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Detomidine carboxylic acid Cat. No.: HY-B0163 Cat. No.: HY-135895

Detomidine produce dose-dependent sedative and Detomidine carboxylic acid is the major urinary effects, is a nonnarcotic, synthetic metabolite of Detomidine. Detomidine is a α2-adrenergic agonist Target: α2-adrenergic synthetic α2-adrenergic agonist and an animal agonist Detomidine is an imidazole derivative and analgesic sedative. Detomidine also has cardiac α2-adrenergic agonist, used as a large animal and respiratory effects and an antidiuretic sedative, primarily used in horses. action. Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Detomidine hydrochloride hydrochloride ((+)- Cat. No.: HY-B0163A hydrochloride; (S)-Medetomidine hydrochloride) Cat. No.: HY-17034A

Detomidine hydrochloride produce dose-dependent Dexmedetomidine Hydrochloride is an agonist of sedative and analgesic effects, is a nonnarcotic, adrenergic alpha-2 receptor, which is used in synthetic α2-adrenergic agonist Target: veterinary medicine for its analgesic and sedative α2-adrenergic agonist Detomidine is an imidazole properties. derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in… Purity: 99.82% Purity: 98.54% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

Diacetolol D7 Dicentrine Cat. No.: HY-100635S Cat. No.: HY-N6969

Diacetolol D7 is a deuterium labeled Diacetolol. Dicentrine is a natural product isolated from the Diacetolol is the major metabolite of Acebutolol. plant Lindera megaphylla with antihypertensive

Diacetolol is a β-adrenoceptor blocking and effect. Dicentrine is an α1-adrenoceptor anti-arrhythmic agent. antagonist which has effective against human hyperplastic .

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

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DL-Epinephrine DL-Norepinephrine hydrochloride ((±)-Epinephrine; DL-; (±)-Adrenaline) Cat. No.: HY-B0447 Cat. No.: HY-N7142

DL-Epinephrine is the racemate of epinephrine. DL-Norepinephrine hydrochloride is a synthetic L-Epinephrine is a hormone secreted by the medulla phenylethylamine that mimics the sympathomimetic of the adrenal glands. L-Epinephrine is an actions of the endogenous α-adrenergic and β-adrenergic receptor agonist. norepinephrineDL-Norepinephrine hydrochloride is a targets α1 and β1 adrenoceptors, has an increasing effect… Purity: >99.0% Purity: 99.53% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 1 g, 5 g Size: 10 mM × 1 mL, 100 mg

Dobutamine hydrochloride hydrochloride Cat. No.: HY-15746 (FPL60278AR) Cat. No.: HY-U00205

Dobutamine hydrochloride is a synthetic Dopexamine hydrochloride is a β2 adrenergic catecholamine that acts on α1-AR, β1-AR, β2-AR receptor agonist. (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR.

Purity: 99.47% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg

Doxazosin D8 (UK 33274) Cat. No.: HY-B0098 (UK 33274 D8) Cat. No.: HY-B0098S

Doxazosin (UK 33274) is a quinazoline-derivative Doxazosin D8 (UK 33274 D8) is a deuterium labeled that selectively antagonizes postsynaptic Doxazosin (UK 33274). Doxazosin is a α1-adrenergic receptors. quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors.

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Doxazosin mesylate (UK 33274 mesylate) Cat. No.: HY-B0098A Cat. No.: HY-101691

Doxazosin mesylate (UK 33274) is a Ecastolol is a beta adrenergic receptor quinazoline-derivative that selectively antagonist, with activities. antagonizes postsynaptic α1-adrenergic receptors.

Purity: 98.60% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g Size: 1 mg, 5 mg

Epanolol hydrochloride (Visacor; ICI141292) Cat. No.: HY-U00183 Cat. No.: HY-B1392

Epanolol (Visacor; ICI141292) is a potent Esmolol hydrochloride is a beta adrenergic β-adrenoceptor with a greater receptor blocker. affinity for β1- than β2-adrenoceptors.

Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

10 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Falintolol, (Z)- Tosylate Cat. No.: HY-U00283 Cat. No.: HY-U00402

Falintolol, (Z)-, a new β-, is Fenmetozole Tosylate is an antagonist of the characterized by the presence of an oxime actions of ethanol, also antagonizes α2-adrenergic function. receptor, and acts as an antidepressant drug.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Fenoterol hydrobromide (Th-1165; Phenoterol) Cat. No.: HY-B0976 (Fenoterol bromide; Th-1165a; Phenoterol hydrobromide) Cat. No.: HY-B0976A

Fenoterol is a β 2 adrenergic agonist designed to Fenoterol hydrobromide is a β 2 adrenergic agonist open up the airways to the lungs, is classed as designed to open up the airways to the lungs, is sympathomimetic β2 agonist and asthma medication. classed as sympathomimetic β2 agonist and asthma medication.

Purity: >98% Purity: 99.71% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 100 mg

Fenspiride Hydrochloride Fiduxosin Cat. No.: HY-A0027 Cat. No.: HY-U00399

Fenspiride Hcl is an α adrenergic and H1 histamine Fiduxosin is a potent α1-adrenoceptor antagonist, receptor antagonist. IC50 value: Target: with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for Adrenergic receptor; H1 receptor Fenspiride α1a-, α1b-, and α1d-adrenoceptors, respectively. hydrochloride is a with anti-inflammatory properties.

Purity: 99.03% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 5 mg

Formoterol Fumarate G-Protein antagonist peptide () Cat. No.: HY-B0010 Cat. No.: HY-P1376

Formoterol fumarate(Foradil) is a potent, G-Protein antagonist peptide is the substance selective and long-acting β2-adrenoceptor agonist. P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors. Purity: 98.94% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 1 mg, 5 mg

G-Protein antagonist peptide TFA Glaucine Cat. No.: HY-P1376A (O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396) Cat. No.: HY-N3945

G-Protein antagonist peptide TFA is the substance Glaucine (O,O-Dimethylisoboldine) is an alkaloid P-related peptide that inhibits binding of G isolated from Glaucium flavum Crantz with proteins to their receptors. G-Protein antagonist antitussive, bronchodilation and anti-inflammatory peptide TFA competitively and reversibly inhibits properties. M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

www.MedChemExpress.com 11

Gramine Acetate (Donaxine) Cat. No.: HY-N0166 (BR-750; Wy8678 acetate) Cat. No.: HY-B0566

Gramine (Donaxine) is a natural alkaloid isolated Guanabenz (Acetate) (BR-750) is an alpha-2 from giant reed, acts as an active adiponectin selective adrenergic agonist used as an

receptor (AdipoR) agonist, with IC50s of 3.2 and antihypertensive agent. 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Purity: 99.45% Purity: 98.88% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 500 mg

Guanfacine hydrochloride Cat. No.: HY-17416A Cat. No.: HY-17416

Guanfacine is a selective α2A receptor agonist. Guanfacine hydrochloride, an anti-hypertensive Target: α2A Receptor Guanfacine is a agent, is a selective α2A-adrenoceptor agonist . It is a selective α2A receptor with Kd of 31 nM and displays 60-fold selectivity agonist. over α2B-adrenoceptors. IC50 Value: 31 nM(Kd) Target: Adrenergic Receptor Guanfacine is a sympatholytic. Purity: >98% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Guanoxabenz (Hydroxyguanabenz) Cat. No.: HY-U00123 (Norcoclaurine) Cat. No.: HY-N2037

Guanoxabenz is an α2 adrenergic receptor Higenamine (Norcoclaurine), a β2-AR agonist, is a agonist. key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine (Norcoclaurine) has anti-apoptotic effects. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 20 mg

Higenamine hydrochloride HOKU-81 (Norcoclaurine hydrochloride) Cat. No.: HY-N2037A (4-Hydroxytulobuterol) Cat. No.: HY-50291

Higenamine hydrochloride (Norcoclaurine HOKU-81, a new bronchodilator, is one of the hydrochloride), a β2-AR agonist, is a key metabolites of . IC50 Value: Target: component of the Chinese herb aconite root that Adrenergic Receptor Effects of HOKU-81 on isolated prescribes for treating symptoms of heart failure trachea and atria of guinea pigs were compared in the oriental Asian countries. with those of various .

Purity: 99.04% Purity: >95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 10 mM × 1 mL, 5 mg, 25 mg

Hydrocortisone 17-butyrate (Cortisol 17-butyrate; Hydrocortisone butyrate) Cat. No.: HY-B0983 Cat. No.: HY-100637

Hydrocortisone 17-butyrate is an adrenocortico Hydroxybupropion is the major active metabolite of hormone. . Hydroxybupropion is metabolized by CYP2B6.Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits

norepinephrine uptake with an IC50 value of 1.7 μM. Purity: 99.93% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 200 mg Size: 1 mg, 5 mg

12 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

ICI 118,551 hydrochloride hydrochloride (ICI 118551 hydrochloride) Cat. No.: HY-13951 (RX 781094 hydrochloride) Cat. No.: HY-14561A

ICI 118,551 (hydrochloride) is a highly selective Idazoxan hydrochloride (RX 781094 hydrochloride)

β2 adrenergic receptor antagonist, with Kis of is an α2-adrenoceptor antagonist and is also a 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, imidazoline receptors (IRs) antagonist respectively. competitively antagonized the centrally induced hypotensive effect of imidazoline-like (IMs). Purity: 99.64% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Imoxiterol (RP 58802B) Cat. No.: HY-101585 Cat. No.: HY-14299

Imoxiterol (RP 58802B) is a β-adrenergic agonist. Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist. IC50 value: Target: β-adrenoceptor Indacaterol inhibits cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors with pEC50 of 8.06. Purity: >98.0% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

Indacaterol maleate (QAB149) Cat. No.: HY-14299A Cat. No.: HY-101717

Indacaterol (QAB149) maleate is an Indanidine is an alpha-adrenergic agonist. ultra-long-acting β-adrenoceptor agonist.

Purity: 99.92% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

Indoramin D5 Isoferulic acid (Indoramine D5; Wy-21901 D5) Cat. No.: HY-12760S (3-Hydroxy-4-methoxycinnamic acid) Cat. No.: HY-N0761

Indoramin D5 is deuterium labeled Indoramin, which Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a piperidine antiadrenergic agent. is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to

and activates α1-adrenergic receptors (IC50=1.4 µM)

to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use. Purity: >98% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Isoprenaline hydrochloride hydrochloride (Isoproterenol hydrochloride) Cat. No.: HY-B0468 Cat. No.: HY-B1270

Isoprenaline hydrochloride is a non-selective Isoxsuprine hydrochloride is a beta-adrenergic beta-adrenergic receptor agonist with potent receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ peripheral vasodilator, bronchodilator, and for myometrial and placcntal beta-adrenergic cardiac stimulating activities. receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.

Purity: >99.0% Purity: 98.87% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 200 mg, 1 g Size: 200 mg

www.MedChemExpress.com 13

Ivabradine D3 Hydrochloride Ivabradine D6 hydrochloride Cat. No.: HY-B0162AS1 Cat. No.: HY-B0162AS

Ivabradine D3 Hydrochloride is the deuterium Ivabradine D6 hydrochloride is the deuterium labeled Ivabradine hydrochloride. Ivabradine labeled Ivabradine hydrochloride. Ivabradine

hydrochloride is a new If inhibitor with IC50 of 2.9 hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent. μM, and used as a pure heart rate lowering agent.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Ivabradine hydrochloride JP1302 dihydrochloride Cat. No.: HY-B0162A Cat. No.: HY-103213

Ivabradine hydrochloride is an orally JP1302 dihydrochloride is a selective, high bioavailable, hyperpolarization-activated, cyclic affinity antagonist of the alpha2C-adrenoceptor

nucleotide-gated (HCN) . (α2C-adrenoceptor), with a Kb value

(antagonist activity) of 16 nM and a Ki (binding affinity) value of 28 nM.

Purity: 99.87% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg, 5 mg

Ko-3290 KUL-7211 racemate Cat. No.: HY-101721 Cat. No.: HY-19673A

Ko-3290 is an antagonist of β-adrenoceptor, with KUL-7211 racemate is the racemate of KUL-7211. cardioselectivity and antilipolytic effects in KUL-7211 is a selective β-adrenoceptor agonist. animals.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

L-(-)-α- L-(-)-α-Methyldopa (hydrate) (MK-351; Methyldopa) Cat. No.: HY-B0225 (MK-351 hydrate; Methyldopa hydrate) Cat. No.: HY-B0225B

Methyldopa is an alpha-adrenergic agonist L-(-)-α-Methyldopa hydrate is an alpha-adrenergic (selective for α2-adrenergic receptors) agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or psychoactive drug used as a sympatholytic or antihypertensive. antihypertensive.

Purity: >98% Purity: >98.0% Clinical Data: Launched Clinical Data: Launched Size: 500 mg Size: 10 mM × 1 mL, 500 mg, 1 g

L-(-)-α-Methyldopa hydrochloride L-765314 (MK-351 hydrochloride; Methyldopa hydrochloride) Cat. No.: HY-B0225A Cat. No.: HY-101385

L-(-)-α-Methyldopa hydrochloride is an L-765314 is a potent and selective α1b adrenergic

alpha-adrenergic agonist (selective for receptor antagonist with Kis of 5.4 nM and 2.0 nM α2-adrenergic receptors) psychoactive drug used as for rat and human α1b adrenergic receptor, a sympatholytic or antihypertensive. respectively.

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 500 mg Size: 1 mg, 5 mg

14 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

L-771688 L-Epinephrine Bitartrate ((-)-Epinephrine (+)-bitartrate Cat. No.: HY-U00237 salt; L-Adrenaline (+)-bitartrate salt) Cat. No.: HY-B0447A

L-771688 is a highly selective α1A-Adrenoceptor L-Epinephrine bitartrate is an α-adrenergic and antagonist with a Ki of 0.43±0.02 nM. β-adrenergic receptor agonist. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands.

Purity: >98% Purity: >99.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g

L755507 hydrochloride Cat. No.: HY-19334 (AH-5158 hydrochloride; Sch-15719W) Cat. No.: HY-B1108

L755507 is a potent, selective agonist of β3-AR Labetalol hydrochloride is a mixed alpha/beta with an IC50 of 35 nM. adrenergic antagonist that is used to treat high blood pressure.

Purity: >98.0% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 10 mM × 1 mL, 100 mg

Landiolol hydrochloride dihydrochloride (ONO1101 hydrochloride) Cat. No.: HY-100607A (Dimebolin dihydrochloride) Cat. No.: HY-14537

Landiolol hydrochloride (ONO1101 hydrochloride) is Latrepirdine dihydrochloride is a neuroactive a highly beta1 selective ultra-short acting compound with antagonist activity at beta-blocker (β1/β2 selectivity=255:1, a , α-adrenergic, and serotonergic half-life of 4min) acts as an adrenoceptor receptors. Latrepirdine stimulates amyloid antagonist. precursor protein (APP) catabolism and amyloid-β (Aβ) secretion. Purity: 99.96% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

Levalbuterol Levalbuterol tartrate ((R)-Albuterol; (R)-; ) Cat. No.: HY-B1675 (Levosalbutamol tartrate) Cat. No.: HY-17457

Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a Levosalbutamol tartrate(levalbuterol) is the short-acting β2-adrenergic receptor agonist R-enantiomer of the short-acting β2-adrenergic and the active (R)-enantiomer of Salbutamol. receptor agonist salbutamol. IC50 Value: Target: Levalbuterol is a more potent bronchodilator than β2-adrenergic receptor Levosalbutamol and Salbutamol and has the potential for the treatment salbutamol produced significantly better of COPD.
. bronchodilator responses than placebo. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Levobetaxolol hydrochloride ((S)-Betaxolol hydrochloride; AL-1577A) Cat. No.: HY-B0381B (ZK-33839) Cat. No.: HY-101815

Levobetaxolol hydrochloride is a beta-adrenergic Lidanserin (ZK-33839) acts as a 5-HT2A and receptor inhibitor (beta blocker), used to lower α1-adrenergic receptor antagonist. the pressure in the eye in treating conditions such as glaucoma.

Purity: 98.11% Purity: >98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg

www.MedChemExpress.com 15

Lofexidine hydrochloride Cat. No.: HY-B1052A (Baq-168; MDL-14042) Cat. No.: HY-B1052

Lofexidine is a selective α2-receptor agonist, Lofexidine (hydrochloride) is a selective commonly used to alleviate the physical symptoms α2-receptor agonist, commonly used to alleviate of heroin and other types of withdrawal. the physical symptoms of heroin and other types of opioid withdrawal.

Purity: 99.08% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg Size: 1 mg, 5 mg

Lusaperidone LY377604 (R107474) Cat. No.: HY-U00117 Cat. No.: HY-13713

Lusaperidone (R107474) is an α2 adrenergic LY377604 is a human β3-adrenergic receptor

receptor antagonist with Kis of 0.13 and 0.15 nM agonist with an EC50 of 2.4 nM and also a β1-

for α2A and α2C, respectively. and β2-adrenergic receptor antagonist.

Purity: 97.74% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg

Mebeverine D6 Hydrochloride metabolite O-desmethyl Mebeverine Cat. No.: HY-A0078S (O-desmethyl Mebeverine alcohol) Cat. No.: HY-G0008

Mebeverine D6 Hydrochloride is the deuterium Mebeverine metabolite O-desmethyl Mebeverine labeled Mebeverine, which is an antimuscarinic. alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Medetomidine Medetomidine hydrochloride Cat. No.: HY-17034 (MPV785) Cat. No.: HY-17034B

Medetomidine(Domtor) is a potent, highly selective Medetomidine hydrochloride is an agonist of α2-adrenoceptor agonist (Ki values are 1.08 and adrenergic alpha-2 receptor, which is used in 1750 nM for α2- and α1-adrenoceptors veterinary medicine for its analgesic and sedative respectively). properties.

Purity: 99.97% Purity: 99.88% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

Metaproterenol Metaproterenol hemisulfate () Cat. No.: HY-B1276A (Orciprenaline hemisulfate) Cat. No.: HY-B1276

Metaproterenol (Orciprenaline) is a direct-acting Metaproterenol hemisulfate (Orciprenaline sympathomimetic and a β2-adrenergic receptor (β2AR) hemisulfate) is a direct-acting sympathomimetic

agonist with an IC50 of 68 nM. Metaproterenol and a β2-adrenergic receptor (β2AR) agonist with

also has anti-inflammatory activity. an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.

Purity: >98% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg

16 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Metipranolol hydrochloride Cat. No.: HY-16316 Cat. No.: HY-17503

Metipranolol hydrochloride is a non-selective β Metoprolol (Toprol) is a selective β1 receptor adrenergic receptor blocking agent. blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. IC50 value: Target: β1 receptor.

Purity: 99.94% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Metoprolol Succinate Metoprolol Tartrate Cat. No.: HY-17503A Cat. No.: HY-17503B

Metoprolol Succinate (Toprol XL) is a selective β1 Metoprolol is a cardioselective β1-adrenergic receptor blocker used in treatment of several blocking agent. Target: β1- adrenergic Receptor diseases of the cardiovascular system, especially Patients took 50 mg metoprolol twice daily with hypertension. IC50 value: Target: β1 receptor. weekly titration to response or 200 mg twice daily.

Purity: 99.54% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg

MG 1 Midaglizole hydrochloride Cat. No.: HY-U00110 ((±)-DG5128; DG5128) Cat. No.: HY-U00165

MG 1 is an α1 adrenergic receptor antagonist. Midaglizole hydrochloride (DG5128) is a preferential α2-adrenoceptor antagonist. Midaglizole hydrochloride (DG5128) exhibits 7.4

times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Mirabegron hydrochloride (YM178) Cat. No.: HY-14773 (Thymoxamine hydrochloride) Cat. No.: HY-B1435

Mirabegron is a selective β3-adrenoceptor Moxisylyte (hydrochloride) is (alpha 1-blocker) agonist with EC50 of 22.4 nM. antagonist, it can vasodilates cerebral vessels without reducing blood pressure. It is also used locally in the eye to reverse the mydriasis caused by and other sympathomimetic agents.

Purity: 99.08% Purity: 99.96% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 100 mg, 1 g

Nadolol D9 (SQ-11725) Cat. No.: HY-B0804 (SQ-11725 D9) Cat. No.: HY-B0804S

Nadolol (SQ-11725) is a non-selective and orally Nadolol D9 (SQ-11725 D9) is the deuterium labeled active β-adrenergic receptors blocker and is a Nadolol. Nadolol is a non-selective and orally substrate of organic anion transporting active β-adrenergic receptors blocker. polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research. Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 250 mg, 500 mg Size: 1 mg, 5 mg

www.MedChemExpress.com 17

Naftopidil Naminterol (KT-611; BM-15275) Cat. No.: HY-B0391 Cat. No.: HY-101822

Naftopidil (Flivas), a selective α1-adrenergic Naminterol is a phenethanolamine derivative, is a

receptor antagonist or , is an β2 adrenoceptor agonist with bronchodilatory . properties. Naminterol is used for treatment of asthma.

Purity: 98.83% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g, 10 g Size: 1 mg, 5 mg

Naphazoline hydrochloride Cat. No.: HY-B0446 (R 065824) Cat. No.: HY-B0203

Naphazoline hydrochloride is an ocular Nebivolol selectively inhibits β1- adrenergic vasoconstrictor and imidazoline derivative receptor with IC50 of 0.8 nM. Target: β1- sympathomimetic amine. Target: Adrenergic Receptor adrenergic receptor Nebivolol reduces cell Naphazoline hydrochloride is the common name for proliferation of human coronary smooth muscle 2-(1-naphthylmethyl)-2-imidazoline hydrochloride. cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Purity: 98.56% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g, 10 g Size: 1 mg, 5 mg

Nebivolol hydrochloride hydrochloride (R 065824 hydrochloride) Cat. No.: HY-B0203A (BMY-13754; MJ-13754-1) Cat. No.: HY-B1396

Nebivolol hydrochloride selectively inhibits β1- Nefazodone hydrochloride is an antidepressant adrenergic receptor with IC50 of 0.8 nM. Target: drug. β1- adrenergic receptor Nebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Purity: 98.73% Purity: 99.71% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

Nicergoline Norepinephrine Cat. No.: HY-B0702 (Levarterenol; L-Noradrenaline) Cat. No.: HY-13715

Nicergoline is an ergot derivative used to treat Norepinephrine (Levarterenol; L-Noradrenaline) is

senile dementia and other disorders with vascular a β1-selective adrenergic receptor agonist with

origins. Target: Alpha-1A adrenergic receptor EC50 of 5.37 μM. Nicergoline acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle.

Purity: 99.06% Purity: 98.08% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 500 mg

Norepinephrine bitartrate monohydrate (Levarterenol Norepinephrine hydrochloride (Levarterenol hydrochloride; bitartrate monohydrate; …) Cat. No.: HY-13715B L-Noradrenaline hydrochloride) Cat. No.: HY-13715A

Norepinephrine bitartrate monohydrate Norepinephrine hydrochloride (Levarterenol

(Levarterenol bitartrate monohydrate; hydrochloride) is a β1-selective adrenergic

L-Noradrenaline bitartrate monohydrate) is a receptor agonist with EC50 of 5.37 μM.

β1-selective adrenergic receptor agonist with

EC50 of 5.37 μM.

Purity: 99.75% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 500 mg, 1 g, 5 g Size: 1 mg, 5 mg

18 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

NRA-0160 Octopamine hydrochloride Cat. No.: HY-101641 ((±)-p-Octopamine hydrochlorid) Cat. No.: HY-B0528A

NRA-0160 is a selective dopamine D4 receptor Octopamine hydrochloride ((±)-p-Octopamine antagonist, with a Ki value of 0.48 nM and with hydrochlorid) is an endogenous that negligible affinity for dopamine D2 receptor is closely related to norepinephrine, and has

(Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat effects on the adrenergic and

5-HT2A receptor (Ki: 180 nM) and rat α1 systems. adrenoceptor (Ki: 237 nM). Purity: >98% Purity: >99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g

Olanzapine D3 (LY170053) Cat. No.: HY-14541 (LY170053 D3) Cat. No.: HY-14541S

Olanzapine (LY170053) is a selective Olanzapine D3 (LY170053 D3) is the deuterium antagonist with high affinity binding to serotonin labeled Olanzapine.

H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Purity: 99.94% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg, 500 mg Size: 1 mg, 5 mg

OPC-28326 hydrochloride Cat. No.: HY-101610 (Ba 39089) Cat. No.: HY-B1486

OPC-28326 is a selective peripheral vasodilator Oxprenolol hydrochloride (Ba 39089) is an orally and an angatonist of α2-adrenergic receptor, with bioavailable β-adrenergic receptor (β-AR)

Ki of 2040, 285, and 55nM for α2A-, α2B- and antagonist with a Ki of 7.10 nM in a radioligand α2C-adrenoceptors, respectively. binding assay using rat heart muscle.

Purity: >98% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Paliperidone (9-Hydroxyrisperidone) Cat. No.: HY-A0019 Cat. No.: HY-U00019

Paliperidone (9-Hydroxyrisperidone), the major Pamatolol is a cardioselective beta-adrenoceptor active metabolite of , is a without sympathomimetic activity. D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Purity: 99.87% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg

Pardoprunox hydrochloride (SLV-308; DU-126891) Cat. No.: HY-14958 (SLV-308 hydrochloride; DU-126891 hydrochloride) Cat. No.: HY-14958A

Pardoprunox (SLV-308) is a partial dopamine D2 Pardoprunox (SLV-308) hydrochloride is a partial and D3 receptor partial agonist and a serotonin dopamine D2 and D3 receptor partial agonist

5-HT1A receptor agonist, with pEC50s of 8, 9.2, and a serotonin 5-HT1A receptor agonist, with and 6.3, respectively. pEC50s of 8, 9.2, and 6.3, respectively.

Purity: >98% Purity: 98.24% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 19

Pargolol hydrochloride Penbutolol sulfate (Ko 1400 hydrochloride) Cat. No.: HY-101658 ((-)-Terbuclomine) Cat. No.: HY-B1154

Pargolol hydrochloride is a β adrenergic Penbutolol sulfate is able to bind to both beta-1 receptor antagonist. adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker. Penbutolol is a sympathomimetic drugused in the treatment of high blood pressure. Purity: >98% Purity: 99.62% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

Perphenazine D8 Dihydrochloride Cat. No.: HY-A0077 Cat. No.: HY-A0077AS

Perphenazine is a drug, Perphenazine D8 Dihydrochloride is the deuterium

inhibits 5-HT2Areceptor, Alpha-1A adrenergic labeled Perphenazine, which is a typical receptor, Dopamine receptor D2/D3, D2L receptor, antipsychotic drug(5-HT, Dopamine receptor

and Histamine H1 receptor, with Ki values of ligand). 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.

Purity: 99.90% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 1 mg, 5 mg

PF-610355 hydrochloride Cat. No.: HY-14296 Cat. No.: HY-B0431A

PF-610355 is a long-acting inhaled Phenoxybenzamine hydrochloride is a selective

β2-adrenoreceptor agonist, with an EC50 of antagonist of both α-adrenoceptor and 0.26 nM. PF-610355 has the potential for the study calmodulin that is commonly used for the of asthma and COPD. treatment of hypertension, specifically caused by .

Purity: >98% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 200 mg, 500 mg, 1 g

Phentolamine mesylate Phenylephrine ( methanesulfonate) Cat. No.: HY-B0362A ((R)-(-)-Phenylephrine; L-Phenylephrine) Cat. No.: HY-B0769

Phentolamine mesylate is a competitive, reversible (R)-(-)-Phenylephrine is a selective

α-adrenoceptor antagonist with an IC50 between 5 α1-adrenoceptor agonist primarily used as a and 30 nM. decongestant.

Purity: 99.83% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

Phenylephrine hydrochloride ((R)-(-)-Phenylephrine Phenylethanolamine A hydrochloride; L-Phenylephrine hydrochloride) Cat. No.: HY-B0471 Cat. No.: HY-131103

(R)-(-)-Phenylephrine hydrochloride is a selective Phenylethanolamine A acts as a β-adrenergic

α1-adrenoceptor agonist with pKis of 5.86, 4.87 agonist. Phenylethanolamine A is a byproduct

and 4.70 for α1D, α1B and α1A receptors during the synthesis process. respectively.

Purity: 99.95% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

20 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Phenylethanolamine A-D3 Cat. No.: HY-131103S (R6238) Cat. No.: HY-12987

Phenylethanolamine A-D3 is a deuterium labeled Pimozide is a dopamine receptor antagonist,

Phenylethanolamine A. Phenylethanolamine A acts as with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine a β-adrenergic agonist. Phenylethanolamine A is a D2, D3 and D1 receptors, respectively, and also byproduct during the Ractopamine synthesis has affinity at α1-adrenoceptor, with a Ki of 39 process. nM; Pimozide also inhibits STAT3 and STAT5.

Purity: >98% Purity: 99.88% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg

Pimozide D4 (R6238 D4) Cat. No.: HY-12987S (LB-46) Cat. No.: HY-B0982

Pimozide D4 (R6238 D4) is a deuterium labeled Pindolol (LB-46) is a nonselective β-blocker with Pimozide. partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).

Purity: >98% Purity: 99.91% Clinical Data: Phase 4 Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Piperoxan hydrochloride (Benodaine hydrochloride) Cat. No.: HY-100850 Cat. No.: HY-12707

Piperoxan hydrochloride is an α2 adrenoceptor Piribedil is a dopamine D2 receptor (D2R) antagonist. agonist which also displays antagonist property at

hα1A-adrenoceptor (hα1A-AR).

Purity: 99.39% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Piribedil D8 (ET-495 D8) Cat. No.: HY-12707S Cat. No.: HY-B0193

Piribedil D8 is the deuterium labeled Piribedil, Prazosin is an alpha-adrenergic blocker and is a which is an antiparkinsonian agent. sympatholytic drug used to treat high blood pressure and , PTSD, and panic disorder. Target: Adrenergic Receptor Prazosin, is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, andpanic disorder. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Prazosin hydrochloride Cat. No.: HY-B0193A ((±)-Pronethalo) Cat. No.: HY-B1238

Prazosin hydrochloride is an alpha-adrenergic Pronethalol is a non-selective beta-adrenergic blocker and is a sympatholytic drug used to treat blocking agent, protect against and to reverse high blood pressure and anxiety, PTSD, and panic Digitalis-induced ventricular arrhythmias. Target: disorder. beta-adrenergic receptor.

Purity: 99.73% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg

www.MedChemExpress.com 21

Propranolol Propranolol D7 hydrochloride Cat. No.: HY-B0573B Cat. No.: HY-B0573S

Propranolol is a nonselective β-adrenergic receptor Propranolol D7 hydrochloride is a deuterium (βAR) antagonist, has high affinity for the β1AR labeled Propranolol hydrochloride. Propranolol

and β2AR with Ki values of 1.8 nM and 0.8 nM, hydrochloride is a nonselective β-adrenergic respectively. Propranolol inhibits [3H]-DHA receptor (βAR) antagonist, has high affinity for

binding to rat brain membrane preparation with an the β1AR and β2AR with Ki values of 1.8 nM and 0.8

IC50 of 12 nM. nM, respectively. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Propranolol hydrochloride QF0301B Cat. No.: HY-B0573 Cat. No.: HY-101690

Propranolol hydrochloride is a nonselective QF0301B is an α1 adrenergic receptor antagonist β-adrenergic receptor (βAR) antagonist, has high and a low α2 adrenoceptor, 5-HT2A, and histamine

affinity for the β1AR and β2AR with Ki values of H1 receptor blocker. 1.8 nM and 0.8 nM, respectively.

Purity: 99.79% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg, 1 g Size: 1 mg, 5 mg

Rauwolscine hydrochloride (α- hydrochloride; Corynanthidine hydrochloride; Isoyohimbine hydrochloride) Cat. No.: HY-12710A (R 55667) Cat. No.: HY-10791

Rauwolscine hydrochloride is a potent and specific Ritanserin (R 55667) is a highly potent,

α2 adrenergic receptor antagonist with a Ki of 12 relatively selective, orally active, long acting

nM. antagonist of 5-HT2 receptor, with an IC50 of

0.9 nM, less active on Histamine H1, Dopamine

D2, Adrenergic α1, Adrenergic α2 receptors.

Purity: 99.95% Purity: >99.0% Clinical Data: Launched Clinical Data: Phase 2 Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg

Ritodrine hydrochloride Ro 363 (DU21220 hydrochloride) Cat. No.: HY-B0452 Cat. No.: HY-123268

Ritodrine hydrochloride (DU21220 hydrochloride) is Ro 363 is a potent and highly selective a β-2 adrenergic receptor agonist. Target: β-2 β1-adrenoceptor agonist. RO 363 is an effective Adrenergic Receptor Ritodrine is a tocolytic drug, inotropic , and is a cardiovascular used to stop premature labor. modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility. Purity: 99.01% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

Rotigotine Rotigotine Hydrochloride (N-0437; N-0923) Cat. No.: HY-75502 (N-0923 Hydrochloride) Cat. No.: HY-A0007

Rotigotine (N-0437; N-0923) is a full agonist of Rotigotine Hydrochloride (N-0923 Hydrochloride) is dopamine receptor, a partial agonist of the a full agonist of dopamine receptor, a partial 5-HT1A receptor, and an antagonist of the agonist of the 5-HT1A receptor, and an

α2B-adrenergic receptor, with Kis of 0.71nM, antagonist of the α2B-adrenergic receptor, with Ki 4-15nM, and 83nM for the dopamine D3 receptor of 0.71nM, 4-15nM, and 83nM for the dopamine D3 and D2, D5, D4 receptors, and dopamine… receptor and D2, D5, D4 receptors, and dopamine… Purity: 99.98% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg

22 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

RS 17053 hydrochloride Salbutamol (RS-17053) Cat. No.: HY-101336 (Albuterol; AH-3365) Cat. No.: HY-B1037

RS 17053 hydrochloride is a potent and selective Salbutamol is a short-acting β2-adrenergic

α1A adrenoceptor antagonist, with a pKi value receptor agonist used for the relief of of 9.1 in native cell membrane and a pA2 value bronchospasm in conditions such as asthma and of 9.8 in functional assays. chronic obstructive pulmonary disease (COPD).

Purity: 99.25% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Salbutamol hemisulfate (Albuterol hemisulfate; AH-3365 hemisulfate) Cat. No.: HY-B0436 (GR33343X) Cat. No.: HY-14302

Salbutamol Hemisulfate (Albuterol hemisulfate) is Salmeterol is a long-acting beta2-adrenergic a short-acting β2 adrenergic receptor agonist receptor (beta 2AR) agonist used clinically to Target: β2 Adrenergic Receptor Salbutamol treat asthma. Hemisulfate (Albuterol hemisulfate) is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and… Purity: >98.0% Purity: 99.68% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Salmeterol xinafoate Salmeterol-D3 (GR 33343X xinafoate) Cat. No.: HY-17453 Cat. No.: HY-135119

Salmeterol xinafoate is a long-acting beta-2 Salmeterol-D3 is the deuterium labeled Salmeterol adrenergic receptor (β2AR) agonist, with Ki of (HY-14302). Salmeterol is a long-acting

1.5 nM for WT β2AR, and used for asthma beta2-adrenergic receptor agonist that is used for treatment. the study of asthma and chronic obstructive pulmonary disease (COPD).

Purity: 99.88% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg, 5 mg

Scopine Scopine hydrochloride (6,7-Epoxytropine) Cat. No.: HY-B0459 (6,7-Epoxytropine hydrochloride) Cat. No.: HY-B0459A

Scopine is the metabolite of , which is a Scopine hydrochloride (6,7-Epoxytropine α1-adrenergic receptor agonist and used in the hydrochloride) is the metabolite of anisodine, treatment of acute circulatory shock. which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.

Purity: >98% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Sertindole (Lu 23-174) Cat. No.: HY-14543 (Org-8282) Cat. No.: HY-32329

Sertindole, a neuroleptic, is one of the newer Setiptiline (Org-8282) is a serotonin receptor antipsychotic available. Target: antagonist. Setiptiline is a tetracyclic Multi-target In vitro studies showed that antidepressant (TeCA) which acts as a sertindole exerts a potent antagonism at serotonin noradrenergic and specific serotonergic 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic antidepressant (NaSSA). receptors. Purity: 99.76% Purity: 96.54% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 23

Silodosin (KAD 3213; KMD 3213) Cat. No.: HY-10122 (GW 427353) Cat. No.: HY-19436

Silodosin (KAD 3213; KMD 3213) is a potent, Solabegron (GW 427353) is a selective

selective and orally active α1A-adrenergic receptor β3-adrenergic receptor agonist, stimulating cAMP (α1A-AR) blocker. accumulation in Chinese hamster ovary cells

expressing the human β3-AR, with an EC50 value of 22 nM.

Purity: 99.96% Purity: 99.91% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg

Sotalol D6 hydrochloride hydrochloride Cat. No.: HY-B0437AS (MJ 1999) Cat. No.: HY-B0437

Sotalol D6 hydrochloride is a deuterium labeled Sotalol hydrochloride (MJ 1999) is a non-selective Sotalol hydrochloride. Sotalol hydrochloride is a competitive β-adrenergic receptor antagonist that non-selective competitive β-adrenergic receptor also exhibits Class III antiarrhythmic properties antagonist that also exhibits Class III by its inhibition of potassium channels. antiarrhythmic properties by its inhibition of potassium channels. Purity: >98% Purity: 99.77% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Spirendolol SR59230A (Li 32-468; S 32-468; Substance 32468) Cat. No.: HY-101817 Cat. No.: HY-100672

Spirendolol is a β adrenergic receptor SR59230A is a potent, selective, and blood-brain antagonist. barrier penetrating β3-adrenergic receptor

antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 50 mg

SR59230A hydrochloride Cat. No.: HY-103200 (Oxedrine) Cat. No.: HY-N0132

SR59230A hydrochloride is a potent, selective, and Synephrine (Oxedrine) is an α-adrenergic and blood-brain barrier penetrating β3-adrenergic β-adrenergic agonist derived from the Citrus

receptor antagonist with IC50s of 40, 408, and aurantium, it has sympathomimetic and 648 nM for β3, β1, and β2 receptors, respectively. structural similarities to ephedra and .

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg

Synephrine hydrochloride dihydrochloride (Oxedrine hydrochloride) Cat. No.: HY-N0132A (B-HT 920 dihydrochloride) Cat. No.: HY-A0008

Synephrine hydrochloride (Oxedrine hydrochloride) Talipexole dihydrochloride (B-HT 920 is an α-adrenergic and β-adrenergic agonist derived dihydrochloride) is a dopamine D2 receptor from the Citrus aurantium, it has agonist, α2-adrenoceptor agonist and 5-HT3 sympathomimetic and structural similarities to receptor antagonist, which displays ephedra and ephedrine alkaloids. antiParkinsonian activity.

Purity: 99.83% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Tamsulosin hydrochloride Cat. No.: HY-B0661 ((R)-(-)-YM12617; LY253351) Cat. No.: HY-B0661A

Tamsulosin is a selective α1 receptor antagonist. Tamsulosin hydrochloride((R)-(-)-YM12617;LY253351) Target: α1 receptor Tamsulosin is a selective α1 is a selective α1 receptor antagonist. Target: α1 receptor antagonist that has preferential receptor Tamsulosin is a selective α1 receptor selectivity for the α1A receptor in the antagonist that has preferential selectivity for versus the α1B receptor in the blood vessels. the α1A receptor in the prostate versus the α1B receptor in the blood vessels. Purity: 99.62% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

TD-5471 hydrochloride hydrobromide Cat. No.: HY-19942A (Lu AA 24530 hydrobromide) Cat. No.: HY-101755

TD-5471 hydrochloride is a potent and selective Tedatioxetine hydrobromide acts as a triple full agonist of the human β2-adrenoceptor. inhibitor and 5-HT2A, 5-HT2C, 5-HT3

and α1A-adrenergic receptor antagonist.

Purity: >98% Purity: 98.44% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Teoprolol Terazosin Cat. No.: HY-U00016 Cat. No.: HY-B0371

Teoprolol is a β-adrenergic receptor blocker. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Terazosin hydrochloride Terazosin hydrochloride dihydrate Cat. No.: HY-B0371F Cat. No.: HY-B0371A

Terazosin hydrochloride is a quinazoline Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and hydrochloride dihydrate works by relaxing blood the opening of the bladder. vessels and the opening of the bladder.

Purity: >98% Purity: 99.85% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Terbutaline sulfate (Terbutaline hemisulfate) Cat. No.: HY-B0802 ((±)​-​Tertatolol; Racemic Tertatolol; dl-​Tertatolol) Cat. No.: HY-U00356

Terbutaline sulfate is a β2-adrenergic receptor Tertatolol is a potent antagonist of agonist; a fast-acting bronchodilator and a beta-adrenoceptor and 5-HT receptor, with tocolytic to delay premature labor. unique renal vasodilatatory effects.

Purity: >98.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 1 mg, 5 mg

www.MedChemExpress.com 25

Tetrahydroalstonine Tetrahydrozoline hydrochloride Cat. No.: HY-N1163 ( hydrochloride) Cat. No.: HY-B0556A

Tetrahydroalstonine, a indole alkaloid isolated Tetrahydrozoline (hydrochloride) is a from the fruits of Rhazya stricta, is a selective α-adrenoceptor agonist. Target: α-adrenoceptor alpha 2-adrenoceptor antagonist. ahydrozoline is an imidazoline derivative with alpha receptor agonist activity widely available in over-the-counter topical ocular and nasal formulations. Purity: 99.95% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg

Tiodazosin (BL-5111) Cat. No.: HY-100255 Cat. No.: HY-B0194

Tiodazosin is a potent competitive postsynaptic Tizanidine is an α2-adrenergic receptor agonist alpha adrenergic receptor antagonist. and inhibits neurotransmitter release from CNS noradrenergic neurons. Target: α2-adrenergic receptor Tizanidine is a drug that is used as a muscle relaxant. It is a centrally acting α2 adrenergic agonist. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Tizanidine hydrochloride Todralazine Cat. No.: HY-B0194A (Ecarazine) Cat. No.: HY-B1001

Tizanidine hydrochloride is an α2-adrenergic Todralazine (Ecarazine) is an anti-hypertensive

receptor agonist and inhibits neurotransmitter agent, acts as a β2AR blocker, with antioxidant release from CNS noradrenergic neurons. Target: and free radical scavenging activity. α2-adrenergic receptor Tizanidine is a drug that is used as a muscle relaxant. It is a centrally acting α2 adrenergic agonist. Purity: 99.48% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Todralazine hydrochloride (Ecarazine hydrochloride) Cat. No.: HY-B1001A (Imidaline; NSC35110) Cat. No.: HY-A0066

Todralazine hydrochloride (Ecarazine Tolazoline(Imidaline) is a non-selective hydrochloride) is an anti-hypertensive agent, acts competitive α-adrenergic receptor antagonist.

as a β2AR blocker, with antioxidant and free radical scavenging activity.

Purity: 98.17% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 500 mg

Tolazoline hydrochloride D8 (Imidaline hydrochloride; NSC35110 hydrochloride) Cat. No.: HY-A0066A Cat. No.: HY-B0532S

Tolazoline (hydrochloride)(Imidaline Trifluoperazine D8 is a deuterium labeled (hydrochloride)) Hcl is a non-selective Trifluoperazine. Trifluoperazine is an competitive α-adrenergic receptor antagonist. antipsychotic agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine is also a potent dopamine D2 receptor inhibitor . Purity: >99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 1 mg, 5 mg

26 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Trifluoperazine dihydrochloride Tropodifene (TFP; SKF5019) Cat. No.: HY-B0532A (Tropaphen) Cat. No.: HY-U00313

Trifluoperazine dihydrochloride (TFP) is an Tropodifene (Tropaphen) is an α-Adrenergic receptor antipsychotic phenothiazine agent and a selective inhibitor. α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is also a potent dopamine D2 receptor inhibitor.

Purity: >99.0% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 1 mg, 5 mg

Tulobuterol Tulobuterol hydrochloride (C-78 free base) Cat. No.: HY-B1810 (C-78) Cat. No.: HY-W011733

Tulobuterol (C-78 free base) is a long-acting Tulobuterol hydrochloride (C-78) is a long-acting

β2-adrenoceptor agonist, which reduces the β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. pulmonary disease and bronchial asthma..

Purity: >98% Purity: 99.82% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 500 mg

Ulimorelin (TZP-101) Cat. No.: HY-14903 Cat. No.: HY-B0716

Ulimorelin (TZP-101) is a receptor (GRLN) Urapidil is an α1 adrenoreceptor antagonist and agonist with an EC50 of 29 nM and a Ki of 16 nM. a 5-HT1A receptor agonist. Ulimorelin is a and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition. Purity: >98% Purity: 99.89% Clinical Data: Phase 3 Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg

Urapidil D6 Urapidil hydrochloride Cat. No.: HY-B0716S Cat. No.: HY-B0354A

Urapidil D6 is a deuterium labeled Urapidil. Urapidil HCl is an α1-adrenoceptor antagonist and Urapidil is an α1-adrenoreceptor antagonist and a 5-HT1A receptor agonist.

5-HT1A receptor agonist.

Purity: >98% Purity: >99.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 25 mg

Vanilpyruvic acid Vatinoxan hydrochloride (Vanylpyruvic acid) Cat. No.: HY-101416 (MK-467 hydrochloride; L-659066 hydrochloride) Cat. No.: HY-19057A

Vanilpyruvic acid is a catecholamine metabolite Vatinoxan hydrochloride (MK-467 and precursor to vanillactic acid. hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.

Purity: >98.0% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 27

Vilanterol trifenatate (GW642444) Cat. No.: HY-14300 (GW642444 trifenatate) Cat. No.: HY-14300A

Vilanterol (GW642444) is a long-acting Vilanterol trifenatate (GW642444 trifenatate) is a

β2-adrenoceptor (β2-AR) agonist with 24 h long-acting β2-adrenoceptor (β2-AR) agonist

activity. The pEC50s for β2-AR,β1-AR and with inherent 24-hour activity. The pEC50s for

β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, β2-AR, β1-AR and β3-AR are 10.37, 6.98 and respectively. 7.36, respectively.

Purity: >98% Purity: 99.02% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Xylazine hydrochloride (BAY 1470) Cat. No.: HY-B0443 (BAY 1470 hydrochloride) Cat. No.: HY-B0443A

Xylazine (BAY 1470) is a strong α2-adrenergic Xylazine hydrochloride (BAY 1470 hydrochloride) is agonist whose effects are mediated via stimulation a strong α2-adrenergic agonist whose effects are of central α2-receptors. Xylazine hydrochloride is mediated via stimulation of central α2-receptors. used as a sedative, analgesic and muscle relaxant Xylazine hydrochloride is used as a sedative, in veterinary medicine. analgesic and muscle relaxant in veterinary medicine. Purity: >98% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

Xylometazoline hydrochloride Yohimbine Cat. No.: HY-B0475 Cat. No.: HY-12715

Xylometazoline hydrochloride is an α-adrenoceptor Yohimbine is a potent and relatively nonselective agonist commonly used as nasal decongestant. alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.

Purity: 99.88% Purity: >98% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 500 mg, 1 g Size: 500 mg

Yohimbine Hydrochloride YS-49 Cat. No.: HY-N0127 Cat. No.: HY-15477

Yohimbine Hydrochloride is an alpha YS-49 is a PI3K/Akt (a downstream target of RhoA) 2-adrenoreceptor antagonist, blocking the pre- and activator, to reduce RhoA/PTEN activation in the postsynaptic alpha-2 adrenoreceptors and causing 3-methylcholanthrene-treated cells. YS-49 inhibits an increased release of noradrenaline and II (Ang II)-stimulated proliferation dopamine. of VSMCs via induction of heme oxygenase (HO)-1.

Purity: 99.85% Purity: 95.38% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g Size: 10 mM × 1 mL, 10 mg, 50 mg

YS-49 monohydrate -d7 Cat. No.: HY-15477A Cat. No.: HY-A0072S

YS-49 (monohydrate) is a PI3K/Akt (a downstream Zilpaterol-d7 is a deuterium labeled Zilpaterol. target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. Purity: >98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 1 mg, 5 mg

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Zinterol ZK-90055 hydrochloride (MJ 9184) Cat. No.: HY-14304 Cat. No.: HY-U00293

Zinterol (MJ 9184) is a potent and selective ZK-90055 hydrochloride is a β2 adrenergic

β2-adrenoceptor agonist. Zinterol increases ICa in receptor agonist. a concentration-dependent manner with an EC50 of 2.2 nM.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg

α1 adrenoceptor-MO-1 β3-AR agonist 1 Cat. No.: HY-U00333 Cat. No.: HY-101514

α1 adrenoceptor-MO-1, an S enantiomer, has β3-AR agonist 1 (compound 15) is a highly potent, affinity at alpha 1 adrenergic receptor, shows selective, and orally available β3-adrenergic alphalytic activity, and possesses analgesic receptor (β3-AR) agonist (EC50=18 nM), being action; more active than R enantiomer. inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

β3-AR agonist 2 Cat. No.: HY-U00391

β3-AR agonist 2 is a potent and selective

β3-adrenergic receptor (β3-AR) agonist with an

EC50 of 8 nM.

Purity: >98% Clinical Data: No Development Reported Size: 1 mg, 5 mg

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