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Androgen Receptor antagonist
(R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells. -
Androgen antagonist
17 alpha-propionate is a new topical and peripherally selective androgen antagonist. -
Androgen Receptor antagonist
Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.- Mirielle C Nauman, .et al. , Cancers (Basel), 2023, Apr 1;15(7):2118 PMID: 37046780
- Mi Chen, .et al. , EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. , Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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RAAS antagonist
Candesartan is an angiotensin receptor blocker (also called an angiotensin-II receptor antagonist or an AIIRA).- Hideki Kobara, .et al. , Molecular Medicine Reports, 2020, 22(2) PMID: 32626983
- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
- Toshihide Kashihara, .et al. , J Physiol, 2017, Jul 1; 595(13): 4207-4225 PMID: 28295363
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AT1 antagonist
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. -
Androgen receptor antagonist
MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.- Shiv Verma, .et al. , Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. , EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. , Mol Carcinog, 2021, Dec 22 PMID: 34939235
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Estrogen receptor antagonist
Tamoxifen Citrateis a selective and potent inhibitor of mammalian sterol isomerase.- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Angiotensin II receptor antagonist
Tasosartan is an angiotensin II receptor antagonist. -
AT1 Antagonist
Telmisartan is an angiotensin II receptor antagonist that inhibits the angiotensin II AT1 receptor.- Chang, YL., .et al. , Cancer Cell Int, 2023, 23(1):111
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AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. -
Estrogen receptor antagonist
(E/Z)-4-hydroxy Tamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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GnRH antagonist
Abarelix acetate is a synthetic peptide gonadotropin releasing hormone receptor (GnRH) antagonist -
Estrogen receptor antagonist
Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.- Marina Arino Martin, .et al. , Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. , Water Res, 2019, Dec 29;171:115451 PMID: 31901682
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GnRH antagonist
Degarelix acetate is a gonadotropin releasing hormone (GnRH) receptor antagonist. -
angiotensin AT2 receptor antagonist
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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GnRH antagonist
Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist. Elagolix inhibits gonadatropin releasing hormone (GnRH) receptors in the pituitary gland and ultimately reduces circulating sex hormone levels. -
androgen-receptor (AR) antagonist
N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors. -
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. -
CRTH2 antagonist
ACT-129968 is a potent and selective CRTH2 antagonist. -
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) -
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. -
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. -
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. -
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. -
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. -
thromboxane A2 (TXA2) receptor (TP receptor) antagonist
Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma. -
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.