Endocrinologie/Hormones

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

ngiotensin II 5-valine is an angiotensin II analog which is an agonist at angiotensin receptors.

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)

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.

2-sec-Butylphenol is an inhibitor of the androgen receptor and P450 aromatase, and can be used in research and experiments in the field of life sciences.

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

AP-238 is a novel synthetic opioid (NSO) that acts as an agonist for the μ-opioid receptor (MOR), with an EC50 of 248 nM. Additionally, AP-238 exhibits analgesic properties.

17-Epiestriol, metabolite of estrone, forms via 16α-hydroxy intermediate and binds ERα and ERβ with affinity less than 17β-estradiol.

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.

ERRγ agonist-2 is a potent and selective ERRγ inverse agonist with a K d value of 6.5 μM.

ZINC05925939 is an estrogen receptor β (ESR2) inhibitor used in breast cancer research.

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.

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

Emd 55068 is a synthetic antagonist of renin.

OP-3633: potent GR antagonist (IC50: 29 nM), low PR agonism, AR antagonism, inhibits GR transcription.

Zankiren is a renin inhibitor. Zankiren can reduce blood pressure, plasma renin activity, and angiotension II.

11-Ketodihydrotestosterone is a metabolite of 11β-Hydroxyandrostenedione. It is an active androgen and is also a potent androgen receptor (AR) agonist (Ki: 20.4 nM, EC50: 1.35 nM for human AR).

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.

4,4'-(Cyclohexylidenemethylene)diphenol (Compound 2) is a symmetrical cyclic non-steroidal estrogen. It exhibits high binding affinity to estrogen receptors ERα and ERβ.

Koreanoside E is a useful organic compound for research related to life sciences. The catalog number is T125538 and the CAS number is 1804014-67-2.