Temocapil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Temocapril 是一种酪氨酸激酶抑制剂。

Temocapril is an inhibitor of?tyrosine kinase.(In Vitro):Temocapril hydrochloride is a prodrug of the ACE inhibitor, Temocaprilat. Temocapril hydrochloride can be readily uptaken via the small intestine, and then be converted to its active metabolite (temocaprilat) by CES1 (human carboxylesterase 1) in the liver.Temocapril hydrochloride (500 nM) reduces the inhibitory effects of RS (N-acetyltetradecapeptide renin substrate) and AngI on neurogenic vasodilation in the SHR.Temocapril hydrochloride (0.1-10 μM; 24 h) shows inductive effects on redox proteins TRX while no effect on antioxidant enzymes Cu/ZnSOD and Mn-SOD expressions.(In Vivo):Temocapril hydrochloride (10 mg/kg; p.o.; 21 d) enhances cardiomyocyte thioredoxin expression and ameliorates autoimmune myocarditis.Temocapril hydrochloride (30 mg/kg; p.o.; daily; for 4 weeks) suppresses Angiotensin I-induced hypertension, plasma and renal ACE activity, but fails to reduce the level of Ang II in the kidney.

Temocapril hydrochloride is a prodrug of the ACE inhibitor, Temocaprilat. Temocapril hydrochloride can be readily uptaken via the small intestine, and then be converted to its active metabolite (temocaprilat) by CES1 (human carboxylesterase 1) in the liver.Temocapril hydrochloride (500 nM) reduces the inhibitory effects of RS (N-acetyltetradecapeptide renin substrate) and AngI (angiotensin) on neurogenic vasodilation in the spontaneously hypertensive rats (SHR).Temocapril hydrochloride (0.1-10 μM; 24 h) shows inductive effects on redox proteins thioredoxin (TRX) while no effect on antioxidant enzymes Cu/ZnSOD and Mn-SOD expressions. Western Blot Analysis Cell Line:Cultured neonatal rat cardiomyocytes Concentration:0.1 μM, 1 μM, 10 μM Incubation Time:24 hours Result:Enhanced redox proteins thioredoxin (TRX) expression 1.9-fold at 10 μM without affecting TRX2, Cu/Zn-SOD or Mn-SOD protein expression.

Temocapril (10 mg/kg; p.o.; 21 d) enhances cardiomyocyte thioredoxin expression and ameliorates autoimmune myocarditis.Temocapril (30 mg/kg; p.o.; daily; for 4 weeks) suppresses Angiotensin I-induced hypertension, plasma and renal ACE activity, but fails to reduce the level of Ang II in the kidney. Animal Model:Experimental autoimmune myocarditis (EAM) rat model Dosage:10 mg/kg Administration:Oral gavage; administration by water; 21 days Result:Ameliorated EAM and prevented cellular proteins from oxidation.Enhanced cardiomyocyte redox regulatory protein TRX expression.Animal Model:Male Sprague Dawley rats Dosage:30 mg/kg Administration:Oral gavage, daily, for 4 weeks Result:Suppressed the blood pressure elevation induced by Ang I.

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Proteasome/Ubiquitin

Tyrosinase

tyrosine kinase

Cardiovascular Disease

hypertension and congestive heart failure diabetic nephropathy

111902-57-9

476.6

C23H28N2O5S2

>98% (HPLC)

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CCOC(=O)C(CCc1ccccc1)NC1CSC(c2cccs2)CN(CC(=O)O)C1=O

14-Thiazepine-4(5H)-acetic acid 6-((1-(ethoxycarbonyl)-3-phenylpropyl)amino)tetrahydro-5-oxo-2-(2-thienyl)- (2S-(2alpha6beta(R*)))-

(-20℃)

With Ice Pack

≥ 2 years