Fimasartan (BR-A-657) is an orally active, highly potent angiotensin II receptor AT1 (AGTR1) antagonist (blocker) that selectively blocks AngII-, but not KCl- or noradrenaline-, induced contraction of rabbit thoracic aortic rings (IC50 = 0.42 nM) with 615-fold higher AT1 affinity than losartan (IC50 = 0.13 nM vs. 80 nM against 0.05 nM AngII for binding rat adrenal cortex). Fimasartan significantly decreases mean arterial blood pressure with rapid onset (in 0.5 h) in spontaneously hypertensive rats (Emax of 75% reduction, 5-24 hr post 10 mg/kg p.o.) and is ~19-fold more effective than losartan against AngII (100 ng/kg i.v.)-induced pressor response in rats in vivo (ED50 = 18 ng/kg vs. 336 ng/kg i.v.).
Orally active, highly potent angiotensin II receptor AT1 (AGTR1) antagonist with superior in vivo antihypertensive efficacy than Losartan.
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Faites votre choix parmi les versions les plus récentes :
Certificats d'analyse (COA)
Lot/Batch Number
It looks like we've run into a problem, but you can still download Certificates of Analysis from our Documents section.
Si vous avez besoin d'assistance, veuillez contacter Service Clients
Déjà en possession de ce produit ?
Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.
Expert opinion on drug metabolism & toxicology, 14(5), 533-541 (2018-04-21)
Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. Fimasartan is a derivative of losartan in which the imidazole ring has been replaced. It provides a selective type 1 angiotensin II receptor antagonist effect with
Archives of pharmacal research, 35(7), 1123-1126 (2012-08-07)
Fimasartan (Kanarb®), an angiotensin II receptor antagonist with selectivity for the AT1 receptor subtype, is a pyrimidinone-related heterocyclic compound that was developed by Boryung Pharm. Co., Ltd. Among numerous synthetic derivatives, fimasartan was chosen as a new drug candidate through
The pharmacological profile of BR-A-657, 2-n-butyl-5-dimethylamino-thiocarbonyl-methyl-6-methyl-3-{[2-(1H-tetrazole-5-yl)biphenyl-4-yl]methyl}-pyrimidin-4(3H)-one, a new nonpeptide AT1-selective angiotensin receptor antagonist, has been investigated in a variety of in vitro and in vivo experimental models. In the present study, BR-A-657 displaced [(125)I][Sar(1)-Ile(8)]angiotensin II (Ang II) from its specific
Journal of clinical pharmacology, 53(1), 75-81 (2013-02-13)
The authors studied the effects of ketoconazole and rifampicin on the pharmacokinetics of a single dose of fimasartan (BR-A-657), a newly developed angiotensin II receptor antagonist for the treatment of hypertension, in 22 healthy participants. Ketoconazole increased the maximumplasma concentration
Journal of cardiovascular pharmacology, 62(2), 229-236 (2013-04-26)
To evaluate the effect of the novel angiotensin receptor blocker Fimasartan on the development of atherosclerosis and plaque stabilization in an animal model. Twenty-four rabbits received an aortic balloon injury from 30 cm to a level just above the aortic
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..
