Fimasartan

Fimasartan is an antagonist of the angiotensin II type 1 (AT1) receptor (IC50 = 0.16 nM in HEK293 cells expressing the human receptor). It is selective for the AT1- over the AT2 receptor (IC50 = 69 µM). Fimasartan (62.5, 125, and 250 µM) inhibits LPS-induced increases in inducible nitric oxide synthase (iNOS) levels and NO production, as well as NF-kappaB nuclear translocation in RAW 264.7 macrophages. It reduces angiotensin II-induced contractions of isolated rabbit aortic rings in a concentration-dependent manner. In vivo, fimasartan decreases mean arterial pressure in rats with hypertension induced by furosemide (Cay-17273) and renal hypertensive rats when administered at doses of 10 and 0.3 mg/kg, respectively. Formulations containing fimasartan have been used in the treatment of hypertension.Formal Name: 2-butyl-1,6-dihydro-N,N,4-trimethyl-6-oxo-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-5-pyrimidineethanethioamide. CAS Number: 247257-48-3. Synonyms: BR-A-657. Molecular Formula: C27H31N7OS. Formula Weight: 501.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 262 nm. SMILES: O=C1C(CC(N(C)C)=S)=C(C)N=C(CCCC)N1CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2. InChi Code: InChI=1S/C27H31N7OS/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26/h7-10,12-15H,5-6,11,16-17H2,1-4H3,(H,29,30,31,32). InChi Key: AMEROGPZOLAFBN-UHFFFAOYSA-N.