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.

PD 117302: nonpeptide, kappa-opioid agonist, anti-arrhythmic, anticonvulsant, impacts locomotion, diuresis.

THR-β agonist 3 is a potent agonist of THR-β.

Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor with anticancer properties.

LY303336 is an antagonist of AT1 receptor.

MCHR1 antagonist 3, a potent antagonist of the melanin-concentrating hormone receptor-1 (MCHR1), is employed for the regulation of energy metabolism.

10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) has neuroprotective effects, can improve cognitive dysfunction, and can be used to study brain injury.

GPR120 Agonist 1 selectively activates human/mouse GPR120 with EC50 of 42/77 nM in HEK293 cells.

CYT-1010, a mu-opioid receptor agonist; EC50: β-arrestin, 13.1 nM; cAMP, 0.0053 nM. Extracted from patent WO2013173730A2.

N-Demethyl Mifepristone (RU 42633), an active metabolite of Mifepristone, exhibits 61% of the affinity for the glucocorticoid receptor relative to Mifepristone'

Firuglipel is an orally available and selective agonist of GPR119.

MCHR1 antagonist 2 is an antagonist of melanin-concentratin hormone receptor 1(MCH1-R, IC50 = 65 nM) and also inhibits hERG.

Halobetasol (Ulobetasol), a corticosteroid, is utilized in the research of severe localized psoriasis [1].

Compound 20, identified as μ opioid receptor agonist 3, is a potent µOR agonist that exhibits an EC50 value of 0.87 nM.

TA-606 is an angiotensin type 1 receptor antagonist with antihypertensive activity.

AMG 837 sodium salt: potent GPR40 agonist, EC50=13 nM; enhances insulin secretion; superior pharmacokinetics.

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and

Fulvestrant R enantiomer is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.

Encaleret( JIT-305) is an antagonist of oral calcium-sensing receptor (CaSR), it is used for the treatment of osteoporosis.

THR-β Modulator-1 (Compound 1a) is a potent modulator of the thyroid hormone receptor β, utilized in the study of thyroid hormone receptor-associated disorders

Fosdagrocorat is an agonist of the dissociated glucocorticoid receptor.

Epelsiban Besylate is an oral drug that is a highly selective anamol oxytocin receptor antagonist.

Glucocorticoid receptor agonist is an effective glucocorticoid receptor agonist.

GPR119 agonist 2 (compound 43), an orally active agonist of GPR119, exhibits favorable pharmacokinetic properties in rodents and has demonstrated efficacy in

EPI-7170: Ralaniten analogue, blocks androgen receptor, inhibits transcription in AR & variants, fights enzalutamide-resistant prostate cancer.

Androgen Receptor Degrader-3 (ARD-3) is a compound that inhibits androgen receptor signaling and promotes the degradation of the receptor, with potential

Biotin-cholesterol, a biotinylated derivative of cholesterol, serves as a precursor in the manufacturing of biotin-conjugated liposomes and micelles, which are utilized in drug delivery systems [1].

"20α-Dihydro Prednisolone, a prednisolone metabolite, is detected in cattle urine post-adrenocorticotropic hormone (ACTH) administration but absent in both naturally stressed and non-stressed cattle."

δ2 opioid receptor antagonist

R-84760, a potent κ-opioid receptor agonist, relieves tonic pain via supraspinal/spinal pathways, activating noradrenergic descent.

AKR1C3-IN-6: Strong AKR1C3 inhibitor (IC50: 0.31 μM); weak on AKR1C2 (IC50: 73.23 μM); shows antitumor effects.

ES 936 is a potent and selective NQO1 inhibitor, inhibiting more than 95% of NQO1 100 nM, with a cell line-dependent inhibition duration.

GPR88-IN-1 is a GPR88 antagonist that may be utilized for the study of central nervous system disorders [1].

Prodilidine hydrochloride is an opioid analgesic.

LX-039: Selective oral estrogen receptor degrader with EC50 of 2.99 nM, antitumor activity, C-3 indole chloride, and robust mouse pharmacokinetics.

nociceptin/orphanin FQ (NOP) receptor antagonist

DPP-4/GPR119 modulator 2 is an inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50: 0.22 μM) and an agonist of GPR119 (EC50: 0.95 μM).

Fulvestrant S enantiomer is the less active S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.

THRβ receptor agonist-1 is an agonist for the THRβ receptor [1].

Nylestriol (LY 49825) is an agonist of estrogen receptor.

DuP-532, an angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension and heart failure.