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Cannabinoid Receptor Cannabinoid Receptor Cannabinoid Receptor Cannabinoid Receptor Cannabinoid receptors are currently classified into three groups: central (CB1), peripheral (CB2) and GPR55, all of which are G-protein-coupled. CB1 receptors are primarily located at central and peripheral nerve terminals. CB2 receptors are predominantly expressed in non-neuronal tissues, particularly immune cells, where they modulate cytokine release and cell migration. Recent reports have suggested that CB2 receptors may also be expressed in the CNS. GPR55 receptors are non-CB1/CB2 receptors that exhibit affinity for endogenous, plant and synthetic cannabinoids. Endogenous ligands for cannabinoid receptors have been discovered, including anandamide and 2-arachidonylglycerol. www.MedChemExpress.com 1 Cannabinoid Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators (S)-MRI-1867 (±)-Ibipinabant Cat. No.: HY-141411A ((±)-SLV319; (±)-BMS-646256) Cat. No.: HY-14791A (S)-MRI-1867 is a peripherally restricted, orally (±)-Ibipinabant ((±)-SLV319) is the racemate of bioavailable dual cannabinoid CB1 receptor and SLV319. (±)-Ibipinabant ((±)-SLV319) is a potent inducible NOS (iNOS) antagonist. (S)-MRI-1867 and selective cannabinoid-1 (CB-1) receptor ameliorates obesity-induced chronic kidney disease antagonist with an IC50 of 22 nM. (CKD). Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg 2-Arachidonoylglycerol 2-Palmitoylglycerol Cat. No.: HY-W011051 (2-Palm-Gl) Cat. No.: HY-W013788 2-Arachidonoylglycerol is a second endogenous 2-Palmitoylglycerol (2-Palm-Gl), an congener of cannabinoid ligand in the central nervous system. 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119. Purity: ≥95.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg (26.4 mM * 100 μL in Acetonitrile), Size: 1 mg, 5 mg 6-Iodopravadoline A-836339 (AM630) Cat. No.: HY-15421 Cat. No.: HY-12761 6-Iodopravadoline (AM630) is a selective CB2 A-836339 is a cannabinoid CB2 receptor-selective antagonist with Ki of 31.2 nM, and displays agonist; exhibits high potencies at CB(2) and 165-fold selectivity over CB1 receptors. selectivity over CB(1) receptors. Purity: 99.58% Purity: 99.61% Clinical Data: No Development Reported 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, 50 mg AM251 AM281 Cat. No.: HY-15443 Cat. No.: HY-13505 AM251 is a selective cannabinoid 1 (CB1) receptor AM281 is a selective CB1 receptor antagonist antagonist with an IC50 of 8 nM, also acts as a with an IC50 of 9.91 nM. AM281 inhibits CB2 potent GPR55 agonist with an EC50 of 39 nM. receptor with an IC50 of 13000 nM. Purity: 98.82% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg AZD1940 BAY 38-7271 Cat. No.: HY-119104 Cat. No.: HY-119744 AZD1940 is an orally active, high affinity BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist with pKi cannabinoid CB1/CB2 receptor agonist, with Kis values of 7.93 and 9.06 for human CB1R and of 1.85 nM and 5.96 nM for recombinant human CB1 CB2R, respectively. AZD1940 shows a robust receptor and CB2 receptor, respectively. BAY analgesia action. 38-7271 has strong neuroprotective properties. Purity: 99.45% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Bay 59-3074 BML-190 Cat. No.: HY-100488 (Indomethacin morpholinylamide; IMMA) Cat. No.: HY-15420 Bay 59-3074 is a selective cannabinoid CB1/CB2 BML-190(IMMA) is a potent and selective CB2 receptor partial agonist with Ki values of 48.3 receptor ligand (Ki values are 435 nM and > 2 and 45.5 nM at human CB1 and CB2 receptors, μM for CB2 and CB1 respectively). respectively. Bay 59-3074 has analgesic properties. Purity: 98.85% Purity: 99.34% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg CB1 antagonist 1 CB1 antagonist 2 Cat. No.: HY-U00397 Cat. No.: HY-116649 CB1 antagonist 1 is an antagonist of CB1 CB1 antagonist 2 is caimabinoid 1 (CB1) receptor, used in the research of metabolic antagonist extracted from patent WO2016184310A1, syndrome and obesity, neuroinflammatory disorders, compound 3, inhibits CB1 in vivo with an IC50 of cognitive disorders and psychosis, 25.5 nM. gastrointestinal disorders, and cardiovascular conditions. Purity: >98% Purity: 99.84% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg CB1-IN-1 CB2 modulator 1 (BPRCB1184) Cat. No.: HY-12790 Cat. No.: HY-135419 CB1-IN-1 (BPRCB1184) is a peripherally restricted CB2 modulator 1 (compound 130) is a potent CB2 CB1R antagonist, with Ki of 0.3 nM and 21 nM for modulator. CB2 modulator 1 has the potential for CB1R (EC50 = 3 nM) and CB2R, respectively. immunedisorders, inflammation, osteoporosis, renal ischemia. Purity: 99.77% 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 CB2R PAM CB2R-IN-1 Cat. No.: HY-131004 Cat. No.: HY-100328 CB2R PAM is an orally active cannabinoid type-2 CB2R-IN-1 is a potent cannabinoid CB2 receptor receptors (CB2Rs) positive allosteric modulator. inverse agonist with a Ki of 0.9 nM. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Drinabant EHP-101 (AVE1625) Cat. No.: HY-14788 (VCE-​004.8) Cat. No.: HY-128872 Drinabant (AVE1625) is an orally active CB1 EHP-101 (VCE-004.8) is an orally active, specific receptor antagonist. Drinabant (AVE1625) inhibits PPARγ and CB2 receptor dual agonist. EHP-101 the agonist-stimulated calcium signal with IC50 inhibits prolyl-hydroxylases (PHDs) and activates values of 25 nM and 10 nM for the hCB1-R and the HIF pathway. EHP-101, a semi-synthetic rCB1-R, respectively, and is ineffective for the multitarget cannabinoquinoid, has potent hCB2-R. anti-inflammatory activity. Purity: >98% Purity: 98.56% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg www.MedChemExpress.com 3 GW842166X Hemopressin (human, mouse) Cat. No.: HY-14167 Cat. No.: HY-P1091 GW842166X is a potent and selective cannabinoid Hemopressin is a nonapeptide derived from the receptor 2 (CB2) agonist with IC50 values of 63 α1-chain of hemoglobin, is originally isolated and 91 nM for human and rat CB2, respectively. from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Purity: 99.97% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg Hemopressin(human, mouse) TFA Hemopressin(rat) Cat. No.: HY-P1091A Cat. No.: HY-P1090 Hemopressin TFA is a nonapeptide derived from the Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of orally active, selective and inverse agonist of CB1 cannabinoid receptors. CB1 cannabinoid receptors. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg Hemopressin(rat) TFA Ibipinabant Cat. No.: HY-P1090A (SLV319; BMS-646256) Cat. No.: HY-14791 Hemopressin(rat) TFA is a nonapeptide derived from Ibipinabant (SLV319) is a potent, selective and the α1-chain of hemoglobin, is originally isolated orally active antagonist of cannabinoid CB1 from rat brain homogenates. Hemopressin(rat) TFA receptor, with a Ki of 7.8 nM. Ibipinabant shows is orally active, selective and inverse agonist of more than 1000-fold selectivity for CB1 over CB2 CB1 cannabinoid receptors. (Ki=7943 nM). Ibipinabant can be used for the research of obesity and diabetic. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg JD-5037 Leelamine hydrochloride Cat. No.: HY-18697 Cat. No.: HY-110028 JD-5037 is a potent CB1R antagonist with an IC50 Leelamine hydrochloride is a tricyclic diterpene of 1.5 nM. molecule that is extracted from the bark of pine trees. Purity: 98.77% Purity: >98% Clinical Data: No Development Reported Clinical Data: Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg LEI-101 LY2828360 Cat. No.: HY-124283A Cat. No.: HY-16642A LEI-101 is a potent, selective, and orally LY2828360 is a slowly acting but efficacious G bioavailable cannabinoid CB2 receptor agonist, protein-biased cannabinoid (CB2) agonist, with a pEC50 of 8 for hCB2, and a pKi of less than inhibiting cAMP accumulation and activating ERK1/2 4 for hERG.
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