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progesterone receptor antagonist
Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.- Hirad A. Feridooni, .et al. , Am J Physiol Heart Circ Physiol, 2017, Jan 1; 312(1): H46-H59 PMID: 27793852
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angiotensin II receptor antagonist
BIBS39 is a nonpeptide angiotensin II (AII) receptor antagonists that displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor. -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
estrogen receptor modulator
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM). -
androgen receptor modulator
LGD-4033 is an investigational selective androgen receptor modulator for treatment of conditions such as muscle wasting and osteoporosis, currently under development by Ligand Pharmaceuticals. -
FFA4/GPR120 agonist
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. - Angiotensin I is formed by the action of renin on angiotensinogen.
- Angiotensin (1-7) is an endogenous peptide fragment that can be produced from Ang I or Ang II via endo- or carboxy-peptidases respectively.
- Vasso Apostolopoulos, .et al. , Bioorg Chem, 2024, Sep:150:107602 PMID: 38959647
- Angiotensin II (Ang II) is an octapeptide hormone that plays a central role in cardiovascular homeostasis.
- Angiotensin III is a hexapeptide formed as a result of a cleavage at the N-terminus of Angiotensin II, a key factor in the Renin-Angiotensin-Aldosterone (RAAS) system by angiotensinases located in red blood cells and the vascular beds of most tissues.
- Angiotensin 1/2 (1-9) is a peptide (ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE-HIS) containing the amino acids 1-9 that are converted from Angiotensin I/II peptide.
- Michaela Lellig, .et al. , J Intern Med, 2024, Nov;296(5):435-448 PMID: 39385670
- Acetyl Angiotensinogen (1-14),porcine, The protein encoded by the Angiotensinogen gene is known as pre-angiotensinogen or angiotensinogen precursor.
- Angiotensin 1/2 (1-5) is a peptide that contains the amino acids 1-5 and is converted from Angiotensin I/II.
- Angiotensin 1/2 (1-6) is a peptide that contains the amino acids 1-6 and is converted from Angiotensin I/II peptide.
- Michaela Lellig, .et al. , J Intern Med, 2024, Nov;296(5):435-448 PMID: 39385670
- Angiotensin 1/2 + A (2 - 8), potent endogenous vasoconstrictor peptide; derivative of angiotensin (Ang) II.
- BNP (1-32), human is a brain natriuretic peptide secreted by the human heart in response to cardiac volume or pressure.
- Parathyroid hormone (PTH) is the most important endocrine regulator of calcium and phosphorus concentration in extracellular fluid, which is secreted by the chief cell of the parathyroid glands as a polypeptide containing 84 amino acids.
- A Vieira-Neto, .et al. , J Dairy Sci, 2021, Jan;104(1):1018-1038 PMID: 33162070
- Deoxycholic acid, extracted from Pig bile, Suitability:Ethanol,ether,three oxygen methane,acetone,acetic acid,alkali hydroxide and alkali carbonate solution.
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Estrogen modulator
Bazedoxifene is a third generation selective modulator of estrogen receptor. -
GnRH agonist
Leuprolide acetate is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors. -
TRβ agonist
Sobetirome is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively to TRβ-1 with EC50 of 0.16 μM. -
Progesterone receptor agonist
Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins. -
Estrogen receptor modulator
Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. -
Renin inhibitor
VTP-27999 2,2,2-trifluoroacetate is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases. -
Enkephalin-degrading and ACE inhibitor
Spinorphin is an endogenous factor that exhibits inhibitory effects on enkephalin-degrading enzymes. -
GPR139 agonist
JNJ 63533054 is a potent and selective GPR139 agonist with EC50 value of 16nm. -
AT1 receptor antagonist
EXP-3174 (Losartan Carboxylic Acid) is a potent and selective noncompetitive AT1 receptor antagonist with IC50 value of 37 nM.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
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GPR119 agonist
APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119. -
LXRα inhibitor
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects. -
Androgen receptor antagonist
ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.- Syeda Afshan, .et al. , Cancer Med, 2024, Sep;13(18):e70240 PMID: 39300962
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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) - 17-Hydroxyprogesterone is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
- Huo, G, .et al. , Appl. Phys. A, 2020, 126, 111
- Zhang J, .et al. , 3 Biotech, 2020, Feb;10(2):35 PMID: 31988829
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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.
- Etonogestrel is a steroidal progestin used in hormonal contraceptives, most notably the subdermal implant Nexplanon and the vaginal ring NuvaRing.
- Linying Li, .et al. , Pharmaceuticals (Basel), 2022, Oct 3;15(10):1226 PMID: 36297338
- Linying Li, .et al. , J Control Release, 2021, Dec 10;340:188-199 PMID: 34678316


