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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. -
Aromatase inhibitor
Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids. -
Androgen Receptor agonist
Andarine (GTX-007) is an investigational selective androgen receptor modulator (SARM). -
RAAS inhibitor
Benazepril hydrochloride is a non-peptide angiotensin-converting enzyme (ACE) inhibitor. Reduces blood pressure and myocardial hypertrophy in spontaneous hypertensive rats.
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Glucocorticoid Receptor Agonist
Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities. - Betamethasone valerate is a potent glucocorticoid steroid with anti-inflammatory and immunosuppressive properties.
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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
- Budesonide is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis.
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RAAS antagonist
Candesartan is an angiotensin receptor blocker (also called an angiotensin-II receptor antagonist or an AIIRA).- Naomi Fukazawa, .et al. , Pharm Res, 2024, May;41(5):849-861 PMID: 38485855
- 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
- Candesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
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Aromatase Inhibitor
Chrysin is a naturally occurring flavone chemically extracted from the blue passion flower (Passiflora caerulea). It has been shown to induce an anti-inflammatory effect, most likely by inhibition of COX-2 expression and via IL-6 signaling. In rodent in vivo studies, chrysin was found anxiolytic. - Clomifene inhibits estrogen receptors in hypothalamus, inhibiting negative feedback of estrogen on gonadotropin release, leading to up-regulation of the hypothalamic-Cpituitary-Cadrenal axis.
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Androgen Receptor Modulators
Ostarine is an androgen receptor modulator (SARM) - Deflazacort is a glucocorticoid used as an anti-inflammatory and immunosuppressant.
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dual 5alpha-reductase inhibitor
Dutasteride is a dual 5-a reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).- Makoto Ishikawa, .et al. , Sci Rep, 2018, 8: 12851 PMID: 30150786
- Makoto Ishikawa, .et al. , Neuropharmacology, 2016, Dec; 111: 142-159 PMID: 27596950
- Makoto Ishikawa, .et al. , Invest Ophthalmol Vis Sci, 2014, 55(12): 8531-8541 PMID: 25406290
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ACE inhibitor
Enalapril is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. -
RAAS inhibitor
Enalaprilat is the active metabolite of enalapril. It is the first dicarboxylate-containing ACE inhibitor and was developed partly to overcome these limitations of captopril. - Raloxifene is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
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Aromatase inhibitor
Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in post-menopausal women. - Finasteride is a synthetic type II 5α-reductase inhibitor. This enzyme converts testosterone to dihydrotestosterone (DHT).
- Chen CC, .et al. , Anticancer Res, 2017, Dec;37(12):6893-6898 PMID: 29187470
- Flunisolide is a corticosteroid often used to treat allergic rhinitis.The principal mechanism of action of Flunisolide is to activate glucocorticoid receptors, meaning it has an anti-inflammatory action.
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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GPR119 agonist
GSK-1292263 is a novel GPR119 agonist.- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Hydrocortisone is a steroid hormone or glucocorticoid produced by the adrenal gland.
- Xijian Wang, .et al. , 3 Biotech, 2020, Sep;10(9):377 PMID: 32802719
- Huo, G, .et al. , Appl. Phys. A, 2020, 126, 111
- Zhang J, .et al. , 3 Biotech, 2020, Feb;10(2):35 PMID: 31988829
- Xiucui Bao, .et al. , J Anal Methods Chem, 2019, Article ID 5676159
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AT1 antagonist
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. -
ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- Asmaa R. Abdel-Hamed, .et al. , J Med Chem Sci, 2023, 6: 250-268
- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
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Aromatase inhibitor
Letrozole is an Aromatase inhibitor. CGS 20267 is a new non-steroidal compound which potently inhibits aromatase in vitro (IC50 of 11.5 nM) and in vivo (ED50 of 1?€?3 μg/kg p.o.)- WEI LIU, .et al. , Exp Ther Med, 2015, Oct; 10(4): 1297-1302 PMID: 26622481
- Levonorgestrelis a synthetic progesterone analog; binds to the progesterone receptor (relative binding affinities are < 0.02, 7.5, 17, 58 and 323 % for estrogen receptors, glucocorticoid receptors, mineralocorticoid receptors, androgen receptors and progesterone receptors respectively).
- 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
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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
- Megestrol Acetate is a progesterone derivative with antineoplastic properties
- Hong Wang, .et al. , Exp Biol Med (Maywood), 2021, Jul 7 PMID: 34233525
- Meprednisone is a glucocorticoid and a methylated derivative of prednisone
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synthetic glucocorticoid receptor agonist
Methylprednisolone is an apoptosis inducer and was also found to inhibit human small cell lung cancer cell growth in vitro. - Mifepristone, an antioxidant and glucocorticoid receptor antagonist, demonstrates the ability to suppress activation of NFκB, a nuclear transcription factor that affects the expression of various adhesion molecules and several inflammatory genes.
- Shuang Liang, .et al. , Cardiovasc Ther, 2022, Apr 7;2022:7145699 PMID: 35474714
- Olmesartan is an angiotensin II receptor antagonist indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Perindopril Butylamine Salt is an angiotensin-converting enzyme (ACE) inhibitor.
- Prednisolone is a glucocorticoid with the general properties of the corticosteroids.
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Glucocorticoid Receptor agonist
Prednisone reduces mucosal TNF-a production, intestinal permeability and levels of NF-kB expression. -
RNA polymerase inhibitor
Antibiotic; inhibits bacterial RNA polymerase. Prototypical activator of the pregnane X receptor (PXR).- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
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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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estrogen-receptor modulator
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 ?M and 2.6 ?M, respectively. -
mast cell stabilizer
Nedocromil is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade.