Trandolapril

Trandolapril is a prodrug form of the angiotensin-converting enzyme (ACE) inhibitor trandolaprilat (Cay-29577). Trandolapril is converted to trandolaprilat by carboxylesterase 1 (CES1) in human liver microsomes. It inhibits angiotensin I-induced pressor responses in rats and dogs (ID50s = 13.1 and 21.1 µg/kg, respectively) and potentiates the bradykinin-induced depressor response in rats (ED50 = 5.5 µg/kg). Trandolapril (0.1, 0.3, and 1 mg/kg) decreases systolic and diastolic arterial pressure in dogs. It decreases mean arterial pressure (MAP) and left ventricular end-diastolic pressure (LVEDP) in a rat model of heart failure induced by left coronary artery occlusion when administered at a dose of 3 mg/kg. Trandolapril (0.01 and 1 mg/kg) increases survival in stroke-prone spontaneously hypertensive rats fed a high-salt diet. Formulations containing trandolapril have been used in the treatment of hypertension.Formal Name: (2S,3aR,7aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-1H-indole-2-carboxylic acid. CAS Number: 87679-37-6. Synonyms: RU-44570. Molecular Formula: C24H34N2O5. Formula Weight: 430.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 25 mg/ml, Ethanol: 0.25 mg/ml, PBS (pH 7.2): 1 mg/ml. SMILES: [H][C@@]12[C@](N(C([C@@H](N[C@H](C(OCC)=O)CCC3=CC=CC=C3)C)=O)[C@H](C(O)=O)C2)([H])CCCC1. InChi Code: InChI=1S/C24H34N2O5/c1-3-31-24(30)19(14-13-17-9-5-4-6-10-17)25-16(2)22(27)26-20-12-8-7-11-18(20)15-21(26)23(28)29/h4-6,9-10,16,18-21,25H,3,7-8,11-15H2,1-2H3,(H,28,29)/t16-,18+,19-,20-,21?/m0/s1. InChi Key: VXFJYXUZANRPDJ-GNFQLOHCSA-N.