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Home , Acolbifene, Arzoxifene, Brilanestrant, Chlorotrianisene, Clomifene, Cyclofenil

Estrogen /ERR

Estrogen receptors are a group of proteins found inside cells. They are receptors that are activated by the hormone estrogen (17β-). Two classes of exist: ER, which is a member of the nuclear hormone family of intracellular receptors, and GPER (GPR30), which is a member of the rhodopsin-like family of G protein-coupled receptors. The ER's helix 12 domain plays a crucial role in determining interactions with coactivators and corepressors and, therefore, the respective or antagonist effect of the . Different ligands may differ in their affinity for alpha and beta isoforms of the estrogen receptor: estradiol binds equally well to both receptors, , and bind preferentially to the alpha receptor, , and to the beta receptor. Estrogen and its receptors are essential for sexual development and reproductive function, but also play a role in other tissues such as . Estrogen receptors are also involved in pathological processes including cancer, , and . Alternative promoter usage and alternative splicing result in dozens of transcript variants, but the full-length nature of many of these variants has not been determined.

www.MedChemExpress.com 1 Estrogen Receptor/ERR Inhibitors, , Antagonists, Activators & Modulators

(+)-Medicarpin (-)-(S)- Cat. No.: HY-N6052 Cat. No.: HY-100583

(+)-Medicarpin, a pterocarpan, is a type of (-)-(S)-Equol is a high affinity ligand for

isolated from several medicinal plant estrogen receptor β with a Ki of 0.73 nM. species with various biological effects, including Sophora japonica, Zollernia paraensis and Platymiscium yucatamun, Machaerium aristulatum,… Purity: >98% Purity: 98.78% 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, 100 mg

(20S)-Protopanaxatriol (E)-4-Hydroxytamoxifen (20(S)-APPT; g-PPT) Cat. No.: HY-N0835 Cat. No.: HY-16950B

(20S)-Protopanaxatriol is a metabolite of (E)-4-Hydroxytamoxifen, the less active of ginsenoside, works through the glucocorticoid (Z)-4-hydroxytamoxifen, is an estrogen receptor receptor (GR) and oestrogen receptor (ER), and modulator. is also a LXRα inhibitor.

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

(E/Z)-4-Hydroxytamoxifen (E/Z)-GSK5182 Cat. No.: HY-16950A Cat. No.: HY-111226A

(E/Z)-4-Hydroxytamoxifen is a racemic compound of (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen and (Z)-GSK5182 . GSK5182 is a highly isomers. (E/Z)-4-Hydroxytamoxifen is an estrogen selective and orally active inverse agonist of

. estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma. Purity: 99.60% Purity: 98.90% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

(R)-Equol (Rac)- ((+)-Equol) Cat. No.: HY-108414 (EM-343; (Rac)-EM-652) Cat. No.: HY-16023B

(R)-Equol is an agonist of both ERα and ERβ with (Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the

Kis of 27.4 and 15.4 nM, respectively. racemic form of EM652 (estrogen ), has anti-estrogenic and estrogenic activities.

Purity: 99.29% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

(±)-Equol 10β,17β-dihydroxyestra-1,4-dien-3-one Cat. No.: HY-100583A (DHED) Cat. No.: HY-128976

(±)-Equol is the racemate of equol. Equol is a 10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a metabolite of the soy , and -targeting bioprecursor of the main . human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.

Purity: 98.04% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

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27-Hydroxycholesterol 4',2-Dihydroxy-4,6-dimethoxydihydrochalcone Cat. No.: HY-N2371 Cat. No.: HY-N8170

27-Hydroxycholesterol is a selective estrogen 4',2-Dihydroxy-4,6-dimethoxydihydrochalcone, an receptor modulator and an agonist of the X estrogen agonist, shows binding affinity for receptor. bovine uterine estrogen receptor with an IC5050 of 15 μM.

Purity: 99.38% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

4'-Raloxifene-β-D-glucopyranoside 4,4'-Iminodiphenol Cat. No.: HY-135594 Cat. No.: HY-135324

4'-Raloxifene-β-D-glucopyranoside, a metabolite of 4-Propionamidophenol (compound 4a) is an inactive Raloxifene, is a glucuronidated at estrogen receptor ligand based on the the 4' postion. 4'-Raloxifene-β-D-glucopyranoside diphenylamine skeleton. is a selective and orally active estrogen receptor antagonist.

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

4-Hydroxytamoxifen 4--D5 ((Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen) Cat. No.: HY-16950 (4-n-Nonylphenol-2,3,5,6-d4,OD) Cat. No.: HY-131122S

4-Hydroxytamoxifen is a selective estrogen 4-Nonylphenol-D5 (4-n-Nonylphenol-2,3,5,6-d4,OD) receptor modulator (SERM). is the deuterium labeled 4-Nonylphenol. 4-Nonylphenol, a major degradation product of Nonylphenol ethoxylates (NPEOs), is a persistent organic pollutant with endocrine-disrupting properties and exerts estrogenic activity. Purity: 99.95% 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: 1 mg, 5 mg

6-Raloxifene-β-D-glucopyranoside Acolbifene Cat. No.: HY-135595 (EM-652; SCH 57068) Cat. No.: HY-16023A

6-Raloxifene-β-D-glucopyranoside, a derivative of Acolbifene (EM-652), the active metabolite of Raloxifene, is a benzothiophene glucuronidated at EM800, is an orally active pure and the 6' postion. 6-Raloxifene-β-D-glucopyranoside selective estrogen receptor antagonist. is a selective and orally active estrogen Acolbifene (EM-652) inhibits estradiol receptor antagonist. (E2)-induced transcriptional activity of ERα (IC50

= 2 nM) and ERβ (IC50 = 0.4 nM). Purity: >98% Purity: 98.86% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Acolbifene hydrochloride AhR modulator-1 (EM-652 hydrochloride; SCH 57068 hydrochloride) Cat. No.: HY-16023 Cat. No.: HY-135671

Acolbifene (EM-652) hydrochloride, an active AhR modulator-1 (compound 6-MCDF) is a selective metabolite of EM800, is an orally active, and orally active aryl hydrocarbon receptor (AhR) cancer-preventing selective estrogen receptor modulator. AhR modulator-1 inhibits , in modulator (SERM). part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat . Purity: 98.48% Purity: >98% Clinical Data: Phase 3 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

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ARV-471 hydrochloride Cat. No.: HY-138642 (LY 353381 HCl; SERM 3) Cat. No.: HY-13556A

ARV-471 is a best-in-class, orally active Arzoxifene hydrocloride is a selective estrogen estrogen receptor (ER) PROTAC degrader. ARV-471 receptor modulator that is a potent estrogen is developed for the research of . antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum .

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

Avobenzone AZD-9833 Cat. No.: HY-B0316 Cat. No.: HY-136255

Avobenzone, a dibenzoylmethane compound, is one of AZD-9833 is a potent and orally active estrogen the most widely used filters in sunscreens for receptor (ER) antagonist. AZD-9833 is used for skin photoprotection in the UVA band. Avobenzone the study of ER+ HER2-advanced breast cancer. is an that directly binds to estrogen receptor β and acts as an estrogen agonist. Purity: ≥98.0% Purity: 98.20% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

AZD9496 AZD9496 maleate Cat. No.: HY-12870 Cat. No.: HY-12870A

AZD9496 is a potent and selective estrogen AZD9496 maleate is a potent and selective estrogen

receptor (ERα) antagonist with an IC50 of 0.28 receptor (ERα) antagonist with IC50 of 0.28 nM. nM. AZD9496 is an orally bioavailable selective AZD9496 maleate is an orally bioavailable oestrogen receptor degrader (SERD). selective oestrogen receptor degrader (SERD).

Purity: 99.28% Purity: ≥95.0% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 50 mg

Bavachin (Corylifolin) Cat. No.: HY-N0233 (TSE-424) Cat. No.: HY-A0031

Bavachin, a first isolated from seeds of Bazedoxifene (TSE-424) is an oral, BBB-penetrant P. corylifolia, acts as a that selective estrogen receptor modulator

activates the estrogen receptors ERα and ERβ with (SERM), with IC50s of 23 nM and 99 nM for ERα

EC50s of 320 and 680 nM, respectively. and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis.

Purity: 99.94% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Bazedoxifene acetate Bazedoxifene hydrochloride (TSE-424 acetate) Cat. No.: HY-A0036 (TSE-424 hydrochloride) Cat. No.: HY-A0031A

Bazedoxifene acetate (TSE-424 acetate) is an oral, Bazedoxifene hydrochloride (TSE-424 hydrochloride) nonsteroidal selective estrogen receptor modulator is an oral active, BBB-penetrant nonsteroidal

(SERM), with IC50s of 23 nM and 99 nM for ERα selective estrogen receptor modulator (SERM),

and ERβ, respectively. Bazedoxifene acetate can be with IC50s of 23 nM and 99 nM for ERα and ERβ, used for the research of osteoporosis. respectively.

Purity: 99.88% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

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

BHPI Cat. No.: HY-12825 (ARN-810; GDC-0810) Cat. No.: HY-12864

BHPI is a potent inhibitor of nuclear Brilanestrant (ARN-810; GDC-0810) is an orally estrogen–ERα-regulated gene expression; elicits bioavailable selective estrogen receptor degrader sustained ERα-dependent activation of the (SERD) with IC50 of 0.7 nM. endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis. Purity: ≥98.0% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Chlorotrianisene Cholesterol Cat. No.: HY-B2158 Cat. No.: HY-N0322

Chlorotrianisene is a long-acting non-steroidal Cholesterol is the major sterol in mammals and is estrogen and an orally active estrogen receptor makes up 20-25% of structural component of the modulator. Chlorotrianisene exhibits plasma membrane. Plasma membranes are highly antiestrogenic activity. Chlorotrianisene potently permeable to water but relatively impermeable to inhibits the COX-1 and inhibits platelet ions and protons. aggregation in whole . Purity: 99.24% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg Size: 500 mg

Chrysin Clomiphene citrate (5,7-Dihydroxyflavone) Cat. No.: HY-14589 ( citrate) Cat. No.: HY-B0463

Chrysin is one of the most well known estrogen Clomiphene citrate (Clomifene citrate) is a blockers. selective estrogen receptor modulator. Target: Estrogen Receptor/ERR Clomifene citrate (CC) acted as an estrogen antagonist regardless of the concentration of E2 added together.

Purity: 99.75% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g

CMP8 Cat. No.: HY-110392 Cat. No.: HY-N2335

CMP8, a selective ligand for estrogen receptor, Coumestrol, a phytoestrogen present in soybean binds to the mutant estrogen receptor ligand products, exhibits activities against cancers, binding domain (ERLBD). CMP8 exhibits IC50 values neurological disorders, and autoimmune diseases. of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, It suppresses proliferation of ES2 cells with an

MGRERα, hERα and hERβ, respectively. IC50 of 50 μM.

Purity: >98% Purity: 98.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg

Cyclofenil Cat. No.: HY-W011100 Cat. No.: HY-B1403

Cyclofenil is a selective estrogen receptor Dienestrol is a synthetic, non-steroidal estrogen, modulator and an -inducing agent. is an estrogen receptor agonist, for the treatment Cyclofenil shows an inhibitory effect on dengue of menopausal and postmenopausal symptoms. virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity. Purity: ≥95.0% Purity: 96.95% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 50 mg

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Diethylstilbestrol Dihydroresveratrol () Cat. No.: HY-14598 Cat. No.: HY-N3755

Diethylstilbestrol (Stilbestrol), a synthetic Dihydroresveratrol, a potent phytoestrogen, is a used in the treatment of hormone receptor modulator. Dihydroresveratrol menopausal and postmenopausal disorders. exhibits proliferative effects in -independent prostate and breast cancer cells at picomolar and nanomolar concentrations.

Purity: 98.54% Purity: 99.96% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 200 mg, 1 g, 5 g Size: 5 mg, 10 mg, 20 mg

DPN () Cat. No.: HY-12452 (3-Hydroxytamoxifen) Cat. No.: HY-121149

DPN (Diarylpropionitrile) is a non-steroidal Droloxifene, a derivative, is an orally estrogen receptor β (ERβ) selective ligand, with active and selective estrogen receptor

an EC50 of 0.85 nM. DPN has neuroprotective modulator. Droloxifene shows antiestrogenic and effects in a number of neurological diseases. anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells.

Purity: 99.66% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg Size: 5 mg

DY131 (GSK 9089) Cat. No.: HY-15483 (RAD1901) Cat. No.: HY-19822

DY131 (GSK 9089) is a potent and selective ERRγ Elacestrant (RAD1901) is an orally available and ERRβ agonist. DY131displays inactive against selective estrogen receptor degrader (SERD) with

ERRα, ERα and ERβ. DY131 also inhibits Smo IC50s of 48 and 870 nM for ERα and ERβ, signaling. respectively.

Purity: 99.72% Purity: >98% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 1 mg, 5 mg

Elacestrant (S enantiomer) Elacestrant dihydrochloride (RAD1901 S enantiomer) Cat. No.: HY-19822D (RAD1901 dihydrochloride) Cat. No.: HY-19822A

Elacestrant S enantiomer (RAD1901 S enantiomer) is Elacestrant dihydrochloride (RAD1901 an low activity enantiomer of elacestrant. dihydrochloride) is an orally available selective

Elacestrant (RAD1901) is a selective and orally estrogen receptor degrader (SERD) with IC50s of available estrogen receptor (ERR) degrader with 48 and 870 nM for ERα and ERβ, respectively.

IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Purity: >98% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Elacestrant S enantiomer dihydrochloride Enclomiphene citrate ((E)-Clomiphene citrate; (RAD1901 S enantiomer dihydrochloride) Cat. No.: HY-19822B trans-Clomiphene citrate; citrate) Cat. No.: HY-118861A

Elacestrant S enantiomer dihydrochloride (RAD1901 Enclomiphene citrate is a potent and orally active S enantiomer dihydrochloride) is an low activity oestrogen receptor antagonist, with enantiomer of elacestrant dihydrochloride. antioestrogenic property.

Purity: >98% Purity: 98.97% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

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

Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 hydrochloride; trans-Clomiphene D4 hydrochloride; …) Cat. No.: HY-118861S Cat. No.: HY-18719E

Enclomiphene D4 hydrochloride ((E)-Clomiphene D4 Endoxifen is a key active metabolite of tamoxifen hydrochloride; trans-Clomiphene D4 hydrochloride; (TAM) with higher affinity and specificity to Enclomifene D4 hydrochloride) is a deuterium estrogen receptor that also inhibits aromatase labeled Enclomiphene. activity. Endoxifen has the potential for breast cancer study.

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

Endoxifen (E-isomer) Endoxifen E-isomer hydrochloride (E-Endoxifen) Cat. No.: HY-18719D (E-Endoxifen hydrochloride) Cat. No.: HY-18719C

Endoxifen E-isomer (E-Endoxifen), an E-isomer of Endoxifen E-isomer hydrochloride (E-Endoxifen Endoxifen, is an impurity in Endoxifen Z-isomer hydrochloride), an E-isomer of Endoxifen, is an drug substance. Endoxifen E-isomer exhibits impurity in Endoxifen Z-isomer drug substance. antiestrogenic effects. Endoxifen E-isomer hydrochloride exhibits antiestrogenic effects.

Purity: 97.23% Purity: 98.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg

Endoxifen hydrochloride Endoxifen Z-isomer Cat. No.: HY-18719B Cat. No.: HY-18719

Endoxifen hydrochloride is a key active metabolite Endoxifen Z-isomer is the most important Tamoxifen of Tamoxifen (TAM) with higher affinity and metabolite responsible for eliciting the specificity to estrogen receptor that also anti-estrogenic effects of this drug in breast inhibits aromatase activity. Endoxifen cancer cells expressing estrogen receptor-alpha hydrochloride has the potential for breast cancer (ERα). study. Purity: 98.32% Purity: >98% 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, 5 mg, 10 mg

Endoxifen Z-isomer hydrochloride Cat. No.: HY-18719A (7-Dehydroestrone) Cat. No.: HY-B1176

Endoxifen Z-isomer hydrochloride is the most Equilin (7-Dehydroestrone) is an important member important Tamoxifen metabolite responsible for of the large group of oestrogenic substances and eliciting the anti-estrogenic effects of this drug is chemically related to menformon (oestrone). in breast cancer cells expressing estrogen Equilin increases the growth of cortical neurons receptor-alpha (ERα). via an NMDA receptor-dependent mechanism.

Purity: 99.31% Purity: 99.12% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

ERB-196 ERD-308 (WAY-202196) Cat. No.: HY-19468 Cat. No.: HY-128600

ERB-196 is a nonsteroidal selective estrogen ERD-308 is a highly potent PROTAC degrader of receptor-β (ERβ) agonist. estrogen receptor (ER) for ER positive breast cancer treatment.

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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ERRα antagonist-1 ERRγ Inverse Agonist 1 Cat. No.: HY-113960 Cat. No.: HY-114411

ERRα antagonist-1 (Compound A) is a selective and ERRγ Inverse Agonist 1 (Compound 12) is a potent, high affinity estrogen-related receptor α (ERRα) selective and orally bioavailable Estrogen-related antagonist. ERRα antagonist-1 inhibits interaction Receptor grammar (ERRγ) inverse agonist, with an

of ERRα with Proliferator-activated Receptor γ IC50 of 40 nM.

Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. Purity: ≥98.0% 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: 1 mg, 5 mg

Erteberel (LY500307) Cat. No.: HY-18295 Cat. No.: HY-15731

Erteberel (LY500307) is a potent and selective Estetrol, a natural estrogen synthesized

(ERβ) agonist with Ki and exclusively during by the human fetal

EC50 of 1.54 nM and 3.61 nM, respectively. liver, is a selective nuclear estrogen receptor Anti-tumor activities. modulator. Estetrol exerts estrogenic actions on the or the central nervous system but presents antagonistic effects on the breast. Purity: ≥99.0% Purity: 95.46% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 1 mg

Estradiol Estradiol (cypionate) (β-Estradiol; E2; 17β-Estradiol; 17β-Oestradiol) Cat. No.: HY-B0141 Cat. No.: HY-B1100

Estradiol is a vital to the is a 17 β-cyclopentylpropinate maintenance of fertility and secondary sexual of estradiol, inhibits ET-1 synthesis via characteristics in females. Estradiol upregulates estrogen receptor IC50 value: Target: estrogen IL-6 expression through the estrogen receptor β receptor Estradiol cypionate is a synthetic ester, (ERβ) pathway. is a estrogen.

Purity: 99.99% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g Size: 10 mM × 1 mL, 500 mg, 1 g

Estradiol benzoate (β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate) Cat. No.: HY-B1192 Cat. No.: HY-B2245

Estradiol Benzoate (β-Estradiol 3-benzoate), a Estradiol dipropionate is a combined prodrug of estradiol, acts as a steroid sex estrogen-, acts as an estrogen and hormone. It exhibits mild anabolic and metabolic progesterone agonist. properties, and increases blood coagulability.

Purity: 99.89% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g Size: 10 mM × 1 mL, 5 mg, 10 mg

Estradiol valerianate Estriol (β-Estradiol 17-valerate) Cat. No.: HY-B0672 (Oestriol) Cat. No.: HY-B0412

Estradiol valerianate (β-estradiol 17-valerate) is Estriol is an antagonist of the G-protein coupled a synthetic estrogen widely used in combination estrogen receptor in estrogen receptor-negative with other steroid hormones in hormone replacement breast cancer cells. therapy drugs.

Purity: 99.95% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 10 mM × 1 mL, 100 mg, 500 mg

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Estrogen receptor modulator 1 Estrogen receptor modulator 6 Cat. No.: HY-110201 Cat. No.: HY-138690

Estrogen receptor modulator 1 (compound 18) is an Estrogen receptor modulator 6 (compound 3a) is a orally active and selective estrogen receptor selective estrogen receptor (ER) β agonist modulator (SERM), with a pIC50 of 0.46. Estrogen (Ki=0.44 nM). Estrogen receptor modulator 6 receptor modulator 1 induces regression of displays 19-fold selectivity for ERβ over

Tamoxifen-resistant, hormone independent xenograft ERα(Ki=8.4 nM). tumors. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg Size: 1 mg, 5 mg

Estrone Estrone-N-O-C1-amido (E1; Oestrone) Cat. No.: HY-B0234 (ERα ligand 1) Cat. No.: HY-111845

Estrone (E1) is a natural estrogenic hormone. Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone is the main representative of the Estrone-based estrogen ligand, which targets endogenous and is produced by several estrogen receptor α (ERα). Estrone-N-O-C1-amido tissues, especially . Estrone is the (ERα ligand 1) binds to cIAP1 ligand Bestatin via a result of the process of aromatization of linker to form SNIPER. that occurs in fat cells. Purity: 99.86% 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

Estropipate (Piperazine ; Estrone sulfate Ethynyl Estradiol piperazine salt) Cat. No.: HY-B1361 (17α-Ethynylestradiol; Ethynylestradiol) Cat. No.: HY-B0216

Estropipate is a form of estrogen, used to treat Ethynyl Estradiol symptoms of , also used to prevent (17α-Ethynylestradiol;Ethynylestradiol) is an osteoporosis. orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.

Purity: 99.0% Purity: 99.40% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

FLTX1 Cat. No.: HY-119437 (ICI 182780; ZD 9238; ZM 182780) Cat. No.: HY-13636

FLTX1 is a fluorescent Tamoxifen derivative that Fulvestrant (ICI 182780) is a pure antiestrogen can specifically label intracellular and a potent estrogen receptor (ER) antagonist

Tamoxifen-binding sites (estrogen receptors) under with an IC50 of 9.4 nM. Fulvestrant is also a permeabilized and non-permeabilized conditions. GPR30 agonist. Fulvestrant effectively inhibits

the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Purity: 99.71% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

G-1 G15 Cat. No.: HY-107216 Cat. No.: HY-103449

G-1 is a nonsteroidal, high-affinity and selective G15 is a high affinity and selective agonist of GPR30 with a Ki of 11 nM. G-protein-coupled estrogen receptor (GPER/GPR30)

antagonist with a Ki of 20 nM.

Purity: 99.51% Purity: 98.38% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

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GDC-0927 GDC-0927 Racemate (SRN-927) Cat. No.: HY-111484 (SRN-927 Racemate) Cat. No.: HY-111484A

GDC-0927 (SRN-927) is a potent, non-steroidal, GDC-0927 Racemate (SRN-927 Racemate) is a degrader orally bioavailable, selective estrogen receptor of estrogen receptor, potently inhibits ER-α

antagonist. activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.

Purity: 99.98% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 1 mg, 5 mg

Genistin (Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside) Cat. No.: HY-N0595 (R 2323) Cat. No.: HY-101405

Genistin (Genistine), an belonging to Gestrinone (R2323) is a synthetic steroid hormone the phytoestrogen family, is a potent used to treat endometriosis. It inhibits leiomyoma

anti-adipogenic and anti-lipogenic agent. Genistin cells with an IC50 of 43.67 μM. attenuates cellular growth and promotes apoptotic death breast cancer cells through modulation of ERalpha signaling pathway. Purity: ≥98.0% Purity: 99.87% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

Giredestrant Giredestrant (GDC-9545) Cat. No.: HY-109176 (GDC-9545 tartrate) Cat. No.: HY-135903

Giredestrant (GDC-9545), a non-steroidal estrogen Giredestrant tartrate (GDC-9545 tartrate), a receptor (ER) ligand, is an orally active and non-steroidal ER ligand, is an orally active and selective ER antagonist. Giredestrant potently selective estrogen receptor (ER) antagonist. competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Purity: 99.52% Purity: >98% Clinical Data: Phase 1 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Glicoricone GPR30 agonist-1 Cat. No.: HY-N9329 Cat. No.: HY-138686

Glicoricone, a phenolic compound, is isolated from GPR30 agonist-1 is a G protein-coupled receptor a species of licorice. Glicoricone is an inhibitor 30 (GPR30) agonist. GPR30 agonist-1 exerts

of monoamine oxidase (MAO), with an IC50 of vasorelaxant effects. 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity.

Purity: >98% Purity: 98.89% 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

GSK-4716 GSK5182 Cat. No.: HY-33353 Cat. No.: HY-111226

GSK-4716 is a selective ERRβ/γ agonist. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ

(ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα.

Purity: 98.83% 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

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

GW7604 Gypenoside XVII Cat. No.: HY-117153 (Gynosaponin S) Cat. No.: HY-N0553

GW7604 is an antiestrogen. GW7604 is the Gypenoside XVII, a novel phytoestrogen belonging metabolite of GW5638, which is a high affinity to the gypenosides, can activate estrogen estrogen receptor (ER) antagonist. receptors.

Purity: ≥98.0% Purity: 99.63% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg Size: 5 mg, 10 mg

H3B-5942 H3B-6545 Cat. No.: HY-112611 Cat. No.: HY-112596

H3B-5942 is a selective, irreversible and orally H3B-6545 is an oral, selective estrogen receptor active estrogen receptor covalent antagonist, covalent antagonist (SERCA) for the research of inactivates both wild-type and mutant ERα by metastatic ER-positive, HER2-negative breast targeting Cys530, with Kis of 1 nM and 0.41 nM, cancer. respectively.

Purity: 99.31% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

H3B-6545 hydrochloride Cat. No.: HY-112596A Cat. No.: HY-B1662

H3B-6545 hydrochloride is an oral, selective Hexestrol is a nonsteroidal synthetic estrogen, estrogen receptor covalent antagonist (SERCA) with a Ki of 0.06 and 0.06 nM for estrogen for the research of metastatic ER-positive, receptor alpha (ERα) and ERβ. Hexestrol can be HER2-negative breast cancer. used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle. Purity: 99.16% 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, 50 mg

Idoxifene Isocurcumenol (CB7432) Cat. No.: HY-U00178 Cat. No.: HY-N4121

Idoxifene (CB7432) is a novel tissue-specific Isocurcumenol, an (ERα) selective estrogen receptor modulator (SERM). inhibitor isolated from Curcuma zedoaria

Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, 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

Kaempferide (Kaempferol 4'-O-methyl ether) Cat. No.: HY-15449 (Kempferol; Robigenin) Cat. No.: HY-14590

Kaempferide is an O-methylated flavonol, a type of Kaempferol (Kempferol), a flavonoid found in many chemical compound. It can be found in Kaempferia edible plants, inhibits estrogen receptor α galanga (aromatic ginger). expression in breast cancer cells and induces apoptosis in cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer. Purity: 99.42% Purity: 99.62% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg

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Lasofoxifene Tartrate Lindleyin (CP-336156) Cat. No.: HY-A0038 Cat. No.: HY-N2448

Lasofoxifene Tartrate is a non-steroidal selective Lindleyin, isolated from Rhei rhizoma, mediates estrogen receptor modulator (SERM). hormonal effects through estrogen receptors. Lindleyin binds to ERα with estrogenic activity.

Purity: 99.80% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg

Liquiritigenin LSZ-102 (4',7-Dihydroxyflavanone) Cat. No.: HY-N0377 Cat. No.: HY-111486

Liquiritigenin, a isolated from LSZ-102 is a potent, orally bioavailable selective

Glycyrrhiza uralensis, is a highly selective estrogen receptor degrader with an IC50 of 0.2

estrogen receptor β (ERβ) agonist with an EC50 nM. of 36.5 nM for activation of the ERE tk-Luc.

Purity: 99.49% Purity: 99.69% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

LY117018 Cat. No.: HY-116896 Cat. No.: HY-B0390

LY117018, a Raloxifene analog, is a selective Mestranol is an inactive prodrug and becomes estrogen receptor modulator. LY117018 exerts biologically active on conversion to ethinyl antiproliferative effects on breast cancer cell estradiol (EE). Mestranol acts as an estrogen lines. receptor agonist.

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

MK-6913 MPP dihydrochloride (Tetrahydrofluoroene 52) Cat. No.: HY-100327 Cat. No.: HY-103454

MK-6913 (Tetrahydrofluoroene 52) is a potent and MPP dihydrochloride is a highly selective selective estrogen receptor β agonist. estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα.

Purity: >98% Purity: ≥99.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 25 mg

N-Desmethyltamoxifen N-Desmethyltamoxifen hydrochloride Cat. No.: HY-129099 Cat. No.: HY-129099A

N-Desmethyltamoxifen is the major metabolite of N-Desmethyltamoxifen hydrochloride is the major tamoxifen in humans. N-Desmethyltamoxifen, a poor metabolite of tamoxifen in humans. antiestrogen, is a ten-fold more potent protein N-Desmethyltamoxifen, a poor antiestrogen, is a kinase C (PKC) inhibitor than Tamoxifen. ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen.

Purity: >98% Purity: 99.62% 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, 100 mg

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

Nitromifene NNC45-0781 (CI628) Cat. No.: HY-100266 Cat. No.: HY-U00216

Nitromifene is an antagonist of estrogen NNC45-0781 is a tissue-selective estrogen receptor (ER). partial-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

OP-1074 Cat. No.: HY-125263 (FC-1271a) Cat. No.: HY-B0723

OP-1074 is a pure antiestrogen and a selective ER Ospemifene is a non-estrogen selective estrogen degrader (PA-SERD), shows specific antiestrogenic receptor modulator (SERM), with Kis of 380 and activity for ERα and ERβ, inhibits 17β-estradiol 410 nM for estrogen receptor α (ERα) and ERβ,

(E2)-stimulated transcriptional activity with IC50 respectively. Ospemifene can be used for the of 1.6 and 3.2nM, respectively. research of vaginal atrophy and breast cancer.

Purity: >98% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg

Ospemifene D4 PAC (FC-1271a D4) Cat. No.: HY-B0723S Cat. No.: HY-112100

Ospemifene D4 (FC-1271a D4) is a deuterium labeled PAC, consists the ADCs linker and PROTACs, Ospemifene. Ospemifene is a selective and orally conjugated to an antibody. PAC extracts from active estrogen receptor modulator for the patent WO2017201449A1, compound LP2. PAC prevention of osteoporosis with IC50 values of 827 conjugated to an antibody is a more marked nM and 1633 nM for estrogen receptor α (ERα) and estrogen receptor-alpha (ERα) degrader compared to ERβ, respectively. PROTAC (without Ab). Purity: >98% Purity: 98.17% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg

PHTPP hydrochloride Cat. No.: HY-103456 Cat. No.: HY-13724B

PHTPP is a selective estrogen receptor β (ERβ) Pipendoxifene hydrochloride is a selective antagonist with 36-fold selectivity over ERα. estrogen receptor modulator (SERM) that can be used for the research of breast cancer.

Purity: 99.64% 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, 100 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 20 mg

Prinaberel (ERB-041) Cat. No.: HY-14933 (BTS 40542) Cat. No.: HY-B0845

Prinaberel (ERB-041) is a potent and selective Prochloraz is an imidazole antifungal that estrogen receptor (ER) β agonist with IC50s of inhibits ergosterol biosynthesis via inhibition of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, the -dependent 14α-demethylation of respectively. Prinaberel displays >200-fold lanosterol, which results in disruption of the selectivity for ERβ over ERα. fungal cell membrane and cell death.

Purity: 98.62% Purity: 99.32% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 250 mg

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Propyl pyrazole triol PROTAC ER Degrader-3 (PPT) Cat. No.: HY-100689 Cat. No.: HY-128527

Propyl pyrazole triol (PPT) is a selective PROTAC ER Degrader-3 is an intermediate for estrogen receptor alpha (ERα) agonist. The synthesis of PAC. PAC, consists the ADCs linker relative binding affinity of Propyl pyrazole triol and PROTACs, conjugated to an antibody. PAC for ERα (ERα: 49%) around 410 times higher extracts from patent WO2017201449A1, compound LP2. compared with estrogen receptor beta (ERβ: 0.12%).

Purity: 99.11% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 1 mg, 5 mg

PROTAC ER Degrader-4 PROTAC ERRα Degrader-1 Cat. No.: HY-135309 Cat. No.: HY-128838

PROTAC ER Degrader-4 is a PROATC estrogen PROTAC ERRα Degrader-1 comprises a MDM2 ligand receptor (ER) degrader, binding to ER with an binding group, a linker and an estrogen-related IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER receptor alpha (ERRa) binding group. PROTAC ERRα

degradation in MCF-7 cells with an IC50 of 0.3 nM. Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.

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

PROTAC ERRα Degrader-2 PROTAC ERRα ligand 1 Cat. No.: HY-128839 Cat. No.: HY-U00425

PROTAC ERRα Degrader-2 comprises a MDM2 ligand PROTAC ERRα ligand 1 is an estrogen-related

binding group, a linker and an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 receptor alpha (ERRa) binding group. PROTAC ERRα and 2.8 μM for ERRα and ERRγ, respectively. Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.

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

PROTAC ERRα ligand 2 PROTAC ERα Degrader-1 Cat. No.: HY-126351 Cat. No.: HY-112098

PROTAC ERRα ligand 2 is an estrogen-related PROTAC ERα Degrader-1 comprises an ubiquitin E3

receptor α (ERRα) inverse agonist with an IC50 ligase binding group, a linker and a protein

of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) binding group. PROTAC ERα Degrader-1 extracts from displays a ~11-fold improved potency than XCT790 patent WO2017201449A1, compound P1. PROTAC ERα

(IC50=61.3 nM). Degrader-1 is an estrogen receptor-alpha (ERα) degrader. Purity: 99.91% Purity: 99.59% Clinical Data: Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 2 mg, 5 mg, 10 mg

PROTAC ERα Degrader-2 Cat. No.: HY-111846 (W-3566) Cat. No.: HY-B1012

PROTAC ERα Degrader-2 comprises a cIAP1 ligand Quinestrol is a synthetic estrogen, used in binding group, a linker and an estrogen receptor hormone replacement therapy, and occasionally to α (ERα) binding group. PROTAC ERα Degrader-2 is treat breast cancer and . an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells.

Purity: 98.02% Purity: 99.67% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 10 mM × 1 mL, 50 mg

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

Raloxifene Raloxifene 4'-glucuronide (Keoxifene; LY156758 free base; LY139481) Cat. No.: HY-13738 Cat. No.: HY-135582

Raloxifene (Keoxifene) is a benzothiophene-derived Raloxifene 4'-glucuronide is a primary metabolite selective estrogen receptor modulator (SERM). of Raloxifene. Raloxifene 4'-glucuronide formation Raloxifene has estrogen-agonistic effects on bone is mediated mostly by UGT1A10 and UGT1A8. and and estrogen-antagonistic effects on Raloxifene 4'-glucuronide binds to estrogen the breast and uterus. Raloxifene is used for receptor with an IC50 of 370 μM. . breast cancer and osteoporosis research. Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Raloxifene 4-Monomethyl Ether Raloxifene 6-glucuronide Cat. No.: HY-135590 Cat. No.: HY-135581

Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene 6-glucuronide is a primary metabolite Raloxifene derivative that inhibits estrogen of Raloxifene. Raloxifene 6-glucuronide is receptor α. Raloxifene 4-Monomethyl Ether mediated mostly by UGT1A1 and UGT1A8. Raloxifene inhibits MCF-7 cells with an IC50 of 1 μM and a 6-glucuronide binds to estrogen receptor with an pIC50 of 6. IC50 of 290 μM.

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

Raloxifene 6-Monomethyl Ether Raloxifene hydrochloride (Keoxifene hydrochloride; LY156758; Cat. No.: HY-135584 LY139481 hydrochloride) Cat. No.: HY-13738A

Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene hydrochloride (Keoxifene hydrochloride) Raloxifene derivative that inhibits estrogen is a second generation selective and orally receptor α. Raloxifene 4-Monomethyl Ether active estrogen receptor modulator. inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6.

Purity: >98% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 50 mg, 100 mg

Saikosaponin D SAR439859 Cat. No.: HY-N0250 Cat. No.: HY-133017

Saikosaponin D is a triterpene saponin isolated SAR439859 (compound 43d) is an orally active, from Bupleurum, with anti-inflammatory, nonsteroidal and selective estrogen receptor anti-bacterial, anti-tumor, and anti-allergic degrader (SERD). SAR439859 is a potent ER activities; Saikosaponin D inhibits selectin, antagonist and has ER degrading activity with an

STAT3 and NF-kB and activates estrogen EC50 of 0.2 nM for ERα degradation. receptor-β. Purity: 98.76% Purity: 99.25% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Segetalin B SNIPER(ER)-110 Cat. No.: HY-107245 Cat. No.: HY-122825

Segetalin B, a cyclopentapeptide from Vaccaria SNIPER(ER)-110 consists of a cIAP1 ligand and an segetalis, possesses estrogen-like activity. estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER)

protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, 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

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SNIPER(ER)-87 Tamoxifen Cat. No.: HY-129619 (ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen) Cat. No.: HY-13757A

SNIPER(ER)-87 consists of an inhibitor of Tamoxifen (ICI 47699) is an orally active, apoptosis protein (IAP) ligand LCL161 derivative selective estrogen receptor modulator (SERM) that is conjugated to the estrogen receptor α which blocks estrogen action in breast cells and (ERα) ligand 4-hydroxytamoxifen by a PEG linker, can activate estrogen activity in other cells, and efficiently degrades the ERα protein such as bone, liver, and uterine cells.

(IC50=0.097 μM). Purity: >98% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g

Tamoxifen Citrate (ICI 46474; (Z)-Tamoxifen Citrate; Tamoxifen-​d5 trans-Tamoxifen Citrate) Cat. No.: HY-13757 (ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5) Cat. No.: HY-13757AS

Tamoxifen Citrate (ICI 46474) is an orally active, Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled selective estrogen receptor modulator (SERM) Tamoxifen. Tamoxifen (ICI 47699) is an orally which blocks estrogen action in breast cells and active, selective estrogen receptor modulator can activate estrogen activity in other cells, (SERM). Tamoxifen is a potent Hsp90 activator such as bone, liver, and uterine cells. and enhances the Hsp90 molecular chaperone ATPase activity. Purity: 99.92% 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

Tectoridin Cat. No.: HY-N0791 Cat. No.: HY-123047

Tectoridin is a isoflavone isolated from Tibolone is a broad spectrum gonadal steroid Maackia amurensis. Tectoridin is a agonist with progestagenic, androgenic, and phytoestrogen and activates estrogen and thyroid estrogenic activities. Tibolone can be used for hormone receptors. Tectoridin exerts the postmenopausal osteoporosis research. estrogenic effects via ER-dependent genomic pathway and GPR30-dependent nongenomic pathway. Purity: 99.57% Purity: 99.68% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 20 mg Size: 10 mM × 1 mL, 100 mg

Toremifene citrate (Z-Toremifene; NK 622 free base; FC-1157a free base) Cat. No.: HY-B0005A (Z-Toremifene citrate; NK 622; FC-1157a) Cat. No.: HY-B0005

Toremifene (Z-Toremifene) is a second-generation Toremifene citrate (Z-Toremifene citrate) is a selective estrogen-receptor modulator (SERM) second-generation selective estrogen-receptor in development for the prevention of osteoporosis. modulator (SERM) in development for the Toremifene also potent inhibits infectious EBOV prevention of osteoporosis.

Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively. Purity: >98% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

Tracheloside WAY-200070 Cat. No.: HY-N1507 Cat. No.: HY-101271

Tracheloside is an antiestrogenic lignin. WAY-200070 is a selective estrogen receptor β

Tracheloside promotes keratinocyte proliferation (ERRβ) agonist with an IC50 of 2.3 nM. through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing.

Purity: >98% Purity: 99.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 20 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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

XCT790 Cat. No.: HY-10426 Cat. No.: HY-N6678

XCT-790 is a potent and selective inverse agonist is a nonsteroidal estrogenic mycotoxin for ERRα with an IC50 value of 0.37 μM. XCT-790 produced by Fusarium species, which colonizes induces cell death in chemotherapeutic resistant several grains. Zearalenone has low acute cancer cells. XCT-790 (Compound 12) is inactive and carcinogenicity. against ERRγ and the estrogen receptors ERα and ERβ. Purity: 99.66% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 5 mg, 10 mg, 25 mg

Zeranol Zuclomiphene citrate (α-Zearalanol) Cat. No.: HY-N6709 Cat. No.: HY-B1617A

Zeranol, a metabolite of the Zuclomiphene citrate is a cis isomer of Clomiphene zearalenone, is an estrogen receptor agonist. citrate. Zuclomiphene citrate has an Zeranol is used as a growth promoter of livestock antiestrogenic effect and can inhibit the due to its strong estrogenic activity. secretion of (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent. Purity: 99.71% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 5 mg

Zuclomiphene D4 citrate α-Zearalenol Cat. No.: HY-B1617AS Cat. No.: HY-N6710

Zuclomiphene D4 citrate is a deuterium labeled α-Zearalenol is a Mycotoxin with high affinity for Zuclomiphene citrate. Zuclomiphene citrate has an the estrogen receptors (ER), α-Zearalenol is the antiestrogenic effect and can inhibit the derivative of zearalenone (ZEN), causes secretion of luteinizing hormone (LH) more than reproductive disorders in animals, due to its the trans isomer. Zuclomiphene citrate is also an xenoestrogenic effects. orally active hypocholesterolemic agent. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg

β-Estradiol 17-acetate (1,3,5(10)-Estratriene-3,17β-diol 17-acetate) Cat. No.: HY-B0708

β-Estradiol 17-acetate is a metabolite of estradiol. Target: Others β-Estradiol 17-acetate is a metabolite of estradiol.

Purity: 95.64% Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg

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