Endocrinologie/Hormones

4'-Hydroxytamoxifen TFA, a salt form of a metabolite of Tamoxifen, demonstrates higher affinity for ER compared to Tamoxifen itself. This compound induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells.

ERD-1233 is an effective oral PROTAC degrader of the estrogen receptor (estrogen receptor) with a DC50 of 0.9 nM. It plays a crucial role in research involving ER+ breast cancer.

6α-Methylprednisolone 21-hemisuccinate sodium salt (Asmacortone), a water-soluble ester, is used for allergic, cardiac, and hypoxic emergencies.

Protirelin Acetate (TRH Acetate) is a thyrotropin-releasing hormone, stimulating the release of thyrotropin and prolactin from the anterior pituitary.

Dehydroisoandrosterone 3-acetate (Prasterone acetate) is a primary C19 steroid generated by the adrenal cortex.

RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR).

Premarin (Estrone 3-sulfate) is an an estrogen sulfate with neuroprotective actions during traumatic brain injury.

Benazeprilat(CGS 14831) is an orally active active metabolite of Benazepril.Benazeprilat has potent antihypertensive activity and can be used in combination

Norethynodrel, a synthetic hormone, mimics progesterone, treats uterine bleeding/endometriosis, and is used with mestranol as a contraceptive.

Estetrol (Donesta), a fetal liver-synthesized estrogen, selectively modulates estrogen receptors and may ease menopausal symptoms.

ARD-266 is a PROTAC degrader based on the von Hippel-Lindau E3 ligase that induces the degradation of AR proteins and is useful in prostate cancer research.

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

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