Candesartan Cilexetil

Candesartan cilexetil is a prodrug form of the angiotensin II type 1 receptor (AT1) antagonist candesartan (Cay-9003239). Candesartan cilexetil is converted to candesartan by hydrolysis in the gastrointestinal tract. It inhibits the pressor response induced by angiotensin II in normotensive rats (ID50 = 0.069 mg/kg), as well as decreases blood pressure, but not heart rate, in spontaneously hypertensive and two kidney-one clip (2K-1C) and 1K-1C renal hypertensive rats (ED25s = 0.68, 0.03, and 0.23 mg/kg, respectively). Candesartan cilexetil (0.1 mg/kg) reduces stroke incidence and urinary protein excretion in stroke-prone spontaneously hypertensive rats. It prevents stress-induced tyrosine hydroxylase transcription and increases AT2 receptor expression in the ventrolateral thalamic nucleus in cold-restraint stressed spontaneously hypertensive rats when administered at a dose of 10 mg/kg per day. Formulations containing candesartan cilexetil have been used in the treatment of hypertension and heart failure.Formal Name: 2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid, 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester. CAS Number: 145040-37-5. Synonyms: Candesartan M1 Cilexetil, TCV-116. Molecular Formula: C33H34N6O6. Formula Weight: 610.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml, Ethanol: 3 mg/ml. lambdamax: 206, 254, 305 nm. SMILES: O=C(OC(C)OC(C1=CC=CC2=C1N(CC3=CC=C(C4=C(C5=NN=NN5)C=CC=C4)C=C3)C(OCC)=N2)=O)OC6CCCCC6. InChi Code: InChI=1S/C33H34N6O6/c1-3-42-32-34-28-15-9-14-27(31(40)43-21(2)44-33(41)45-24-10-5-4-6-11-24)29(28)39(32)20-22-16-18-23(19-17-22)25-12-7-8-13-26(25)30-35-37-38-36-30/h7-9,12-19,21,24H,3-6,10-11,20H2,1-2H3,(H,35,36,37,38). InChi Key: GHOSNRCGJFBJIB-UHFFFAOYSA-N.