Temocapril HCl

SKU: orb1222873

Description

Temocapril HCl, the hydrochloride of Temocapril, is a long-acting ACE inhibitor used for the therapy of hypertension.(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.

Key Properties

• CAS Number: 110221-44-8
• MW: 513.07
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₈N₂O₅S₂·HCl
• SMILES: CCOC(=O)[C@H](CCc1ccccc1)N[C@H]1CS[C@@H](CN(C1=O)CC(=O)O)c1cccs1.Cl
• Target: ACE
• Solubility: DMSO : ≥ 100 mg/mL; 194.91 mM

Bioactivity

• 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. 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 administration, daily, for 4 weeks. Result: Suppressed the blood pressure elevation induced by Ang I.
• 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 whileno effect on antioxidant enzymes Cu/ZnSOD and Mn-SOD expressions. Cell Proliferation Assay Cell line: Cultured neonatal rat cardiomyocytes. Concentration: 0.1 μM, 1 μM, 10 μM Incubation time: 24 hours. Result: Enhanced TRX protein expression 1.9-fold at 10 μM without affecting TRX2, Cu / Zn-SOD or Mn-SOD protein expression.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

ACE