Endocrinologie/Hormones

ERα/ERβ antagonist-1 (Compound 10) functions as a partial antagonist of both ERα and ERβ. It reduces the activity of ERα and ERβ in HepG2 liver cells in a dose-dependent manner.

TLB 150 Benzoate (RAD150) is a modulator of the androgen receptor with an IC50 value of 0.13 μM.

R4K1 is a cell-permeable stapled peptide that binds with high affinity to estrogen receptor (ER) α, inhibiting its interaction with coactivators. It penetrates breast cancer cells, regulating gene transcription and suppressing cell proliferation. R4K1 is applicable for tumor research.

AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.

CGP-42112 acetate is a potent angiotensin receptor AT2 agonist that inhibits the increase in protein kinase A activity produced by LPS.

ERα degrader 6 (Compound 31q) is an ERα degrader with a K I of 75 nM and also inhibits ARO with an IC50 value of 37.7 nM.

ET Receptor Antagonist 2 (Compound 16j) is an orally active ET receptor antagonist with an IC50 of 0.22 nM, suitable for pulmonary arterial hypertension (PAH)

ERD-3111 (Compound 44), an orally active PROTAC ERα degrader (DC50: 0.5 nM), exhibits efficacy in inhibiting tumor growth in both the parental MCF-7 xenograft

Compound 181, also known as 14-3-3σ/ERα Stabilizer-1, is a covalent stabilizer targeting the 14-3-3σ/ERα proteins.

WCA-814, an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate, induces degradation of both full-length and AR-V7, exhibiting cytotoxic effects in

Androgen Receptor Antagonist 9 (compound 28) serves as an antagonist to the androgen receptor [1].

Anticancer agent 135 (compound 26h) acts as a potent androgen receptor (AR) antagonist, effectively blocking AR nuclear translocation and inhibiting AR/AR-V7

ET Receptor Antagonist 1 (compound 16h), with an IC50 value of 0.18 nM, is an orally active agent that can be utilized for pulmonary arterial hypertension (PAH

"ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH)

Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the

MK-0773 FA (MK-0773 FA (606101-58-0 Free base)) is an androgen receptor modulator used for the prevention and treatment of cancer-related muscle wasting.

Parathyroid Hormone (1-34), bovine is a PTH receptor agonist used to study osteoporosis and hypoparathyroidism.

AMG7703 is a bioactive chemical.

(Rac)-PF-998425: nonsteroidal AR antagonist, potent & selective, IC50: 26 nM (binding), 90 nM (cellular), potential for androgenetic alopecia study.

(R,S)-Ivosidenib is the less active enantiomer of Ivosidenib .

GW-1100 is a selective GPR40 and FFAR1 antagonist for the study of diabetes and metabolic diseases.

BAN ORL 24 dihydrochloride is a highly potent nociceptin/orphan FQ (N/OFQ) receptor (NOP) antagonist that can be used to study neurological diseases.

PD 123319 ditrifluoroacetate is a selective non-peptide AT2 receptor antagonist with IC50 of 34 nM.

GPR40 agonist 6 (Compound 7a) is a potent and selective agonist of free fatty acid receptor 1 ( FFAR1 or GPR40 ) with an EC 50 of 0.058 μM against GPR40 [1].

Azilsartan mepixetil: potent, long-acting angiotensin II blocker, safely lowers blood pressure, protects heart and kidneys.

Monomethyl fumarate D3 is a deuterium labeled Monomethyl fumarate.

AC-186 is an ERβ agonist with neuroprotective activity for the study of Parkinson's disease.

Betamethasone Acetate (Standard) is the standard substance of Betamethasone Acetate, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Betamethasone acetate, the 21-acetate ester of betamethasone, is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.

Angiotensin II (3-8), human is a less effective agonist at the angiotensin AT1 receptor.

Atosiban (RW22164), an oxytocin/vasopressin inhibitor, halts premature labor as an intravenous tocolytic, reducing uterine contractions rapidly.

Tricaprin (Standard) is the standard substance of Tricaprin, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Glycerol Tridecanoate is an orally active precursor (DA precursor) of caprylic acid that can be hydrolyzed to caprylic acid. It is a major component of medium chain triglycerides (MCT) and has antiandrogenic and antihyperglycemic properties. It can be used as an additive in food, pharmaceuticals and cosmetics.

ZQ-16 is a potent GPR84 agonist (EC50=0.213 μM) activating multiple signaling pathways.

TUG-770 is a highly potent agonist of free fatty acid receptor 1 (FFA1/GPR40, EC50: 6 nM for hFFA1).

CGP-42112 is an agonist of the Angiotensin-II subtype 2 receptor (AT2 R).

YE 120 is a GPR35 agonist.

Diflorasone Diacetate, a topical glucocorticoid, has immunosuppressive and anti-inflammatory properties.

Azilsartan (TAK-536) D5 is the deuterium-labeled Azilsartan. Azilsartan is a specific antagonist of the angiotensin II type 1 receptor.

Angiogenin (108-122) peptide treats cancer, infectious, fibrotic, inflammatory, neurodegenerative, autoimmune, and heart diseases.

D4-abiraterone is the active metabolite of abiraterone.Δ4-Abiraterone is a inhibitor of CYP17A1, 3β-HSD and SRD5A, and an antagonist of the androgen receptor.

BMS-986121 is a selective positive allosteric modulator (PAM) of the μ opioid receptor with analgesic effects.

It is an inhibitor of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)

Trans-Diethyl-1,1,1',1'-Stilbestrol-3,3',5,5'-d8 is a deuterated compound of Trans-Diethyl-Stilbestrol. Trans-Diethyl-Stilbestrol has a CAS number of 56-53-1. Diethylstilbestrol is used in the treatment of menopausal and postmenopausal disorders.

Vanillylpyruvic acid is a phenylpyruvic acid derivative applicable in biochemical experiments and drug synthesis research.

Rezvilutamide (SHR3680) is an orally available androgen receptor inhibitor that crosses the blood-brain barrier and has antitumor activity.

GDC-0927 is a novel,non-steroidal, potent, orally bioavailable, selective estrogen receptor antagonist.

Zearalenone is a nonsteroidal estrogenic mycotoxin produced by Fusarium species, which colonizes several grains.

DOCP, a mineralocorticoid, treats dogs with adrenal insufficiency.

ARD-1676 is an orally administered androgen receptor (AR) PROTAC degrader that combines an AR ligand with a cereblon ligand.

Hydrocortisone cypionate is a corticosteroid ester and synthetic glucocorticoid corticosteroid.

ERα degrader-2 is an estrogen receptor (SERD) degrader with anticancer activity that inhibits ERα for the prevention and treatment of HER-positive breast canc