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Merck
CN

SML3256

Fimasartan

≥98% (HPLC)

Synonym(s):

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, 2-n-Butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one, BR-A-657, BR-A657

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About This Item

Empirical Formula (Hill Notation):
C27H31N7OS
CAS Number:
247257-48-3
Molecular Weight:
501.65
UNSPSC Code:
12352107
NACRES:
NA.77
MDL number:
MFCD24369685
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

Key Documents

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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)

SMILES string

S=C(CC1=C(N=C(N(C1=O)CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CCCC)C)N(C)C

InChI key

AMEROGPZOLAFBN-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Related Categories

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Je Hak Kim et al.
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
Fabio Angeli et al.
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
Jong-Young Lee et al.
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
Jung Won Kim et al.
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
Suran Ryu et al.
Biological & pharmaceutical bulletin, 36(3), 467-474 (2013-03-02)
Since inhibition of angiotensin II type 1 (AT1) receptor reduces chronic inflammation associated with hypertension, we evaluated the anti-inflammatory potential and the underlying mechanism of fimasartan, a Korean Food and Drug Administration approved anti-hypertension drug, in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages.
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