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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. -
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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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. -
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. -
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. -
Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- 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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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
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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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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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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.
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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. -
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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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. -
ACE inhibitor
Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.- Tomas Jasenovec, .et al. , Biomedicines, 2021, Dec 14;9(12):1902 PMID: 34944718
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GPR3 agonist/NOS/ NADPH oxidases inhibitor
Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells. -
CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
LTA4 hydrolase inhibitor
Captopril Disulfide is a reversible and competitive inhibitor of LTA4 hydrolase (IC50=11 M). Captopril has been shown to be an of angiotensin converting enzyme-1 (ACE1), but not ACE2(IC50 = 22 nM). -
ACE inhibitor
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. -
Renin inhibitor
VTP-27999 HCl is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin. -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
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. -
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. -
5 alpha-reductase inhibitor
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. -
OC2 inhibitor
CSRM617 Hydrochloride is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice. -
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. -
ACE inhibitor
H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM. -
RORγt inhibitor
S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production. -
Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
ACE inhibitor
Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease. -
angiotensin-converting enzyme inhibitor
Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks. -
Aromatase inhibitor
Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM. -
testosterone 5-alpha-reductase inhibitor
Finasteride (acetate) is an orally active testosterone 5-alpha-reductase inhibitor. -
direct renin inhibitor
Aliskiren D6 Hydrochloride (CGP 60536 D6 Hydrochloride) is is deuterium labeled Aliskiren, which is a direct renin inhibitor with IC50 of 1.5 nM. -
estrogen receptor (ER) inhibitor
WAY-169916 is a pathway-selective inhibitor of estrogen receptor (ER) that acts by inhibiting NF-kB transcriptional activity.