Formulation: A solid
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
Purity: ≥98%
Formula Markup: C27H31N7OS
Formula Weight: 501,6
Shelf life (days): 1460
CAS Number: 247257-48-3
Notes: Fimasartan is an antagonist of the angiotensin II type 1 (AT1) receptor (IC50 = 0.16 nM in HEK293 cells expressing the human receptor).{51311} 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-κB nuclear translocation in RAW 264.7 macrophages.{51312} It reduces angiotensin II-induced contractions of isolated rabbit aortic rings in a concentration-dependent manner.{51311} In vivo, fimasartan decreases mean arterial pressure in rats with hypertension induced by furosemide (Item No. 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.
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