Temocapril  (Synonyms: 替莫普利)

Temocapril is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases^[1][2].

Angiotensin-converting Enzyme (ACE)^[1]

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^[1].
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)^[2].
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^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Temocapril (10 mg/kg; p.o.; 21 d) enhances cardiomyocyte thioredoxin expression and ameliorates autoimmune myocarditis^[3].
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^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

476.61

C₂₃H₂₈N₂O₅S₂

111902-57-9

固体

Off-white to yellow

替莫普利

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Fukami T, et al. In vitro evaluation of inhibitory effects of antidiabetic and antihyperlipidemic drugs on human carboxylesterase activities. Drug Metab Dispos. 2010 Dec;38(12):2173-8.  [Content Brief]

  [2]. Kawasaki H, et al. Angiotensin inhibits neurotransmission of calcitonin gene-related peptide-containing vasodilator nerves in mesenteric artery of spontaneously hypertensive rats. J Pharmacol Exp Ther. 1998 Feb;284(2):508-15.  [Content Brief]

  [3]. Yuan Z, et al. Temocapril treatment ameliorates autoimmune myocarditis associated with enhanced cardiomyocyte thioredoxin expression. Cardiovasc Res. 2002 Aug 1;55(2):320-8.  [Content Brief]

  [4]. Ohnishi K, et al. Angiotensin-converting enzyme inhibitor does not suppress renal angiotensin II levels in angiotensin I-infused rats. J Pharmacol Sci. 2013;122(2):103-8.  [Content Brief]