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5-alpha reductase inhibitor
β-sitosterol reduces blood levels of cholesterol, and is sometimes used in treating hypercholesterolemia. β-Sitosterol inhibits cholesterol absorption in the intestine. When the sterol is absorbed in the intestine, it is transported by lipoproteins and incorporated into the cellular membrane. -
Aromatase inhibitor
Fadrozole is a nonsteroidal aromatase inhibitor exhibiting a very potent and selective inhibitory effect of the aromatase enzyme system in vivo and estrogen biosynthesis in vivo.- Steve U. Ayobahan, .et al. , Sci Rep, 2019, 9, Article number: 6599 PMID: 31036921
- Muth-Köhne E, .et al. , Aquat Toxicol, 2016, Jul;176:116-27 PMID: 27130971
- Ma YN, .et al. , Aquat Toxicol, 2016, Oct;179:55-64 PMID: 27571716
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AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
renin inhibitor
Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren, which is a direct renin inhibitor approved for the treatment of essential hypertension. -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
HMG-CoA Reductase inhibitor
Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.
- ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
- Ruibao Chen, .et al. , Biomed Res Int., 2015, 2015: 514234 PMID: 26491675
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ACE inhibitor/Beta blocker
Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. - Calcifediol-D6 is the deuterated form of Calcifediol(25-hydroxy Vitamin D3), which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 (cholecalciferol) by the enzyme cholecalciferol 25-hydroxylase.
- Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
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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. - Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.
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Glucocorticoid receptor agonist
Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist. - Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.
- Olmesartan medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure. Olmesartan works by blocking the binding of angiotensin II to the AT1 receptors in vascular muscle. By blocking the binding rather than the synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
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Renin inhibitor
Aliskiren is an orally active, synthetic nonpeptide renin inhibitor.- Karibe T, .et al. , Drug Metab Dispos, 2018, May;46(5):667-679 PMID: 29358184
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progesterone receptor agonist
Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.- Xijian Wang, .et al. , 3 Biotech, 2020, Sep;10(9):377 PMID: 32802719
- Xiucui Bao, .et al. , J Anal Methods Chem, 2019, Article ID 5676159
- Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene acetate significantly prevents bone mass loss at 20 mg/day in healthy postmenopausal women with normal or low bone mineral density.
- Renu Sudhakar, .et al. , Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.
- Prednisolone is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
- Meclizine is a human pregnane X receptor (hPXR) agonist. It possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Its antiemetic and antivertigo effects are not fully understood, but its central anticholinergic properties are partially responsible.
- Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I.
- Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme inhibitor (ACE) which is used for the treatment of hypertension and congestive heart failure.
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ACE inhibitor
Cilazapril is a pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure. -
ACE inhibitor
Fosinopril is an angiotensin converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of chronic heart failure. -
AT1 Receptor Blocker
Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension. -
estrogen agonist
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist. - Fluticasone propionate is a high affinity, selective glucocorticoid receptor agonist (Kd = 0.5 nM).
- Abhinav Kumar, .et al. , Pharm Res, 2017, 34(12): 2454-2465 PMID: 28560698
- Imidapril (Tanatril) is an inhibitor of angiotensin converting enzyme (ACE).
- Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes.
- Pregnenolone is an endogenous steroid hormone for inhibition of M1 receptor- and M3 receptor-mediated currents with IC50 of 11.4 μM and 6.0 μM, respectively.
- Liquiritigenin is a plant-derived highly selective estrogen receptor ?? agonist
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Estrogen receptor degrader
Elacestrant (RAD1901) is an orally available selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. -
CB2 inverse agonist
SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.- Ming Tang, .et al. , Cell Death Dis, 2018, Jun; 9(6): 601 PMID: 29789558
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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 - KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.