Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. - Flurandrenolide is a synthetic glucocorticoid with anti-inflammatory and anti-allergic properties. Flurandrenolide exerts its effects by interacting with specific cytoplasmic glucocorticoid receptors and subsequently activates glucocorticoid receptor mediated gene expression.
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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. -
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. -
Androgen Receptor antagonist
EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ?? 6 μM) -
Estrogen receptor degrader
Brilanestrant (GDC-0810, ARN-810??? is a potent ER-α binder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors. -
GnRH agonist
Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. -
SERD/SERM
RAD1901 is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. -
GnRH agonist
Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. - Versipelostatin is a novel GRP78/Bip molecular chaperone down-regulator of microbial origin that was isolated from the metabolite of Streptomyces versipellis strain 4083-SVS6.
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progesterone receptor ligand
Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17?α-hydroxyprogesterone formed from caproic acid. - Protirelin is a thyrotropin-releasing hormone receptor used to treat hypothyroidism.
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Progesterone Receptor Agonist
Desogestrel is a synthetic progestational hormone used often as the progestogenic component of combined oral contraceptive agents. -
GPR139 antagonist
NCRW0005-F05, first antagonist selective for GPR139 (IC50 value 0.21 uM); a useful tool to study GPR139 pharmacology, especially in combination with the GPR139 agonist JNJ 63533054. -
RORγ modulator
RORγ modulator 1 is a retinoid-related orphan receptor gamma (RORy) modulator, extracted from patent WO/2015061515 A1, example 124. - Endoxifen (E-isomer hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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angiotensin II receptor type 1 antagonist
Azilsartan medoxomil is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. - Chlormadinone acetate is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive.
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glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. -
GPR35/CXCR8 agonist
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8. - Vitamin D2 (Ergocalciferol) is a form of vitamin D, used as a vitamin D supplement.
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GPR55 antagonist
CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor. -
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. -
synthetic glucocorticoid receptor agonist
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent. -
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.
