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RORγ agonist
LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist. -
Aldosterone Receptor Antagonist
Esaxerenone, also known as CS-3150, XL-550, is a nonsteroidal antimineralocorticoid that acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone. -
RORγt inhibitor
AGN-242428, also known as VTP-43742, is a potent, selective and orally active RORγt inhibitor for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis. -
ERRβ & ERRγ Agonist
GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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synthetic glucocorticoid receptor agonist
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent. -
Estrogen receptor agonist
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.- Gao X, .et al. , Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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ER antagonist
Fulvestrant S enantiomer is the S enantiomer of Fulvestrant. Fulvestrant is a selective estrogen receptor (ER) antagonist which can be used to treat breast cancer. -
FAA1 agonist
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. - Androsterone is a steroid hormone produced in the body from 5α-reduced metabolites of dehydroepiandrosterone. It is the major androgen excreted in urine as a metabolite of testosterone and is used as the international reference standard for androgenic activity.
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glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
Estrogen receptor ligand
α-Estradiol is an endogenous estrogen receptor ligand (Ki values are 0.2 and 1.2 nM for ERα and ERβ receptors respectively). -
glucocorticoid agonist
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone. - Medroxyprogesterone is used in the treatment of renal carcinoma. It is a synthetic progestational hormone used in veterinary practice as an estrus regulator.
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Androgen receptor antagonist
Spironolactone is a potent antagonist of the androgen receptor. -
non-peptide angiotensin II receptor antagonist
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys. - Estropipate is a form of estrogen, an estrogen receptor agonist. It has several uses such as: Alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics, and treatment of prostate cancer and prevention of osteoporosis.
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glucocorticoid
Fluorometholone is a glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders. -
GnRH/LHRH receptor agonist
Leuprorelin is a Gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, LHRH) receptor agonist. Suppresses estradiol, LH and FSH serum levels and represses the growth of experimental rat endometriosis. -
GnRH agonist
Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. - Gestrinone (R2323) is a synthetic steroid hormone used to treat endometriosis. It inhibits leiomyoma cells with an IC50 of 43.67 μM.
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selective Estrogen receptor modulator
Lasofoxifene tartrate is a third-generation selective estrogen receptor modulator. -
thromboxane A2 (TXA2) receptor (TP receptor) antagonist
Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. -
glucocorticoid receptor agonist
Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma. - Norethindrone acetate is used in combination with estrogen as a contraceptive (oral). It is reasonably anticipated to be a human carcinogen.
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5 alpha-reductase inhibitor
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. -
gonadotropin-releasing hormone agonist
Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist). -
TRH-R agonist
Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release). -
GnRH antagonist
Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment. The IC50 of 1.21 nM. -
OC2 inhibitor
CSRM617 Hydrochloride is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice. -
glucocorticoid receptor agonist
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent. -
aromatase inhibitor
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively. - PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
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ROR agonist
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5. -
Glucocorticoid receptor (GR) antagonist
Exicorilant (CORT 125281) is a selective and oral active glucocorticoid receptor (GR) antagonist, with a Ki value of 7 nM. Exicorilant (CORT 125281) has potential to overcome adiposity, glucose intolerance and dyslipidaemia. -
glucocorticoid
Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid.