Endocrinology/Hormones

AM-1638 is an orally active GPR40/FFA1 agonist, useful for studying type II diabetes.

PF 00277343, a thyroid receptor agonist, is used for the treatment of androgenetic alopecia.

Prinaberel (ERB 041) is an ERβ agonist with anticancer activity and anti-inflammatory activity that inhibits the NFκB pro-inflammatory signaling pathway.

Arzoxifene hydrochloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue.

MOMBA is a selective orthosteric agonist specifically targeting engineered human free fatty acid 2 (hFFA2) receptors, particularly those modified as designer

L-368899: non-peptide, oral oxytocin receptor antagonist (IC50: 8.9 nM), 40x more selective than vasopressin V1a/V2.

MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).

LY2922470: Selective GPR40 agonist; EC50=7nM (human), 1nM (mouse), 3nM (rat); lowers glucose, boosts insulin/GLP-1.

18-Hydroxy-11-deoxy Corticosterone (18-OH-DOC) is a mineralocorticoid produced by the zona fasciculata of the adrenal gland, with its biosynthesis regulated by adrenocorticotropic hormone (ACTH) and angiotensin II. This regulation heightens 18-OH-DOC production in isolated human adrenal glomerulosa cells and allows for its formation from 11-deoxy corticosterone (DOC) in human SK-MEL188 melanoma cells. As an intermediate in progesterone metabolism, 18-OH-DOC can be converted to aldosterone in rat adrenal glands' capsular portion. Its continuous infusion (200 μg/rat per day) has been shown to raise systolic blood pressure in uninephrectomized saline-drinking rats, and elevated plasma levels of 18-OH-DOC have been observed in the adb/db mouse model of type 2 diabetes.

SNC 162 is a potent and selective delta-opioid receptor (δ-opioid) agonist with analgesic, antidepressant and antiarrhythmic effects.

GLL398: Oral ERα down-regulator, binds strongly (IC50=1.14nM), degrades ERα in MCF-7 cells (IC50=0.21μM).

MK-8666, a partial GPCR agonist, targets GPR40 to enhance insulin secretion, potentially treating type 2 diabetes without adverse effects.

Ro 48-6791, a GABA receptor agonist, is used potentially for anesthesia.

Glucocorticoid receptor-IN-1 selectively modulates GR with anti-inflammatory effects, represses hMMP1 (IC50: 2.11 nM), and activates MMTV (EC50: 5.59 nM).

TC OT 39, Oxytocin analog, selective OXTR agonist (EC50=180 nM) and V1aR antagonist, mimics oxytocin-induced scratching.

BI-2081: GPR40 agonist, EC50=4nM, boosts insulin, lowers blood glucose, potential for type 2 diabetes research.

Org 43553: oral LMW LH-R agonist; targets LH (EC50: 3.7nM) & FSH (EC50: 110nM); useful for endocrine research.

Azilsartan mopivabil is the potent antagonist of angiotensin II receptor .

10-Chloroestra-1,4-diene-3,17-dione acts as an estrogen receptor α (ERα) agonist, enhancing reporter gene expression in S.

Biotin-hexanamide-(L-Thyroxine) is a biotinylated derivative of L-Thyroxine (Levothyroxine; T4), utilized as a synthetic hormone in hypothyroidism research [1].

Trimegestone, a highly effective oral progestogen, is used for endometrial protection, all doses inducing secretory endometrial transformation.

SPH3127 is a potent oral direct renin inhibitor, effective at 0.4 nM for human renin, used to study hypertension.

Taragarestrant (D-0502), an oral estrogen receptor degrader, combats ER+ breast cancer in research.

JJH260, a N-hydroxy hydantoin carbamate, inhibits AIG1 and ADTRP with IC50 values of 0.57 μM and 8.5 μM, respectively, and targets ABHD6, LYPLA1/2.

GSK 1440115, an orally active urotensin II receptor antagonist, is used to treat asthma.

(1S,3R)-GNE-502 degrades ERα in MCF7 cells; potent with EC50 of 13 nM; useful in estrogen-related cancer research.

Imlunestrant (LY-3484356) is an orally active, selective estrogen receptor degrader that persistently inhibits ER-dependent gene transcription and cell growth.

RU 59063 is a prototype of a new class of high-affinity nonsteroidal androgen receptor (AR) ligands.

LGD-2941 is an androgen receptor modulator. LGD-2941 is used for the treatment of hypogonadism, female sexual dysfunction and menopausal syndrome.

(+)-Chloroquine, an aminoquinoline drug, inhibits the in vitro terminal glycosylation of angiotensin-converting enzyme 2 (ACE-2) [1].

DXP, a lipophilic prodrug of Dexamethasone, has 47x less glucocorticoid receptor affinity; it's an agonist & anti-inflammatory.

μ opioid receptor agonist 1 (Compound H-1a) is an optically pure oxyheterocyclic substituted pyrroloxypyrazole derivative and an MOR receptor agonist that can

GPR120 Agonist 3 (GPR120-IN-1) is a selective agonist of Gpr120 ( logEC50: -7.62).

L 681176 is an inhibitor of the angiotensin-converting enzyme.

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist that can be used to study diseases caused by endocrine abnormalities.

Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).

μ1 receptor antagonist

BE-26263, an antiosteoporotic agent isolated from Scedosporium apiospermum, exhibits an estrogenic effect [1].

Prostaglandin E2-biotin, an analog of prostaglandin, is utilized in the research of Nurr1-related diseases, including cancer and autoimmune diseases [1].

A81988 is an antagonist of angiotensin AT1 receptors.

ADL-08-0011 is an metabolite of alvimopan.

ZD-8731, an angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension and heart failure.

HP210, a selective glucocorticoid receptor modulator (SGRM), can suppress IL-1β and IL-6 mRNA expression, suggesting its utility in investigating inflammation-

Frakefamide: potent analgesic, μ-selective agonist, non-CNS penetrating.

VPC-14228 is a specific AR-DBD inhibitor that acts by inhibiting both Y594A and Q592A mutants.

IP7e (isoxazolo-pyridinone 7e) is a Nurr1 activator with an EC50 value of 3.9 nM.

Androgen Receptor Degrader-2 (Compound 9) is a potent degrader of androgen receptors, with potential application in cancer research [1].

JNJ-26146900 is a nonsteroidal androgen receptor (AR) ligand with tissue-selective activity in rats. JNJ-26146900 binds to the rat AR with a K(i) of 400nM.

Spirorenone (INN) is a novel aldosterone antagonist with anti-salt corticosteroid activity, used in metabolic disease research.

Elisartan is a non-peptide pro-drug of angiotensin II AT1 receptor antagonist HN-12206. It also shows anti-hypertension activities.