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Fimasartan

Fimasartan structure

CAS No:
247257-48-3
Formula:
C27H31N7OS
Chemical Name:
Fimasartan
Synonyms:
5-Pyrimidineethanethioamide,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-butyl-1,6-dihydro-N,N,4-trimethyl-6-oxo-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-;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;Fimasartan;Kanarb;2-[2-Butyl-4-methyl-6-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-N,N-dimethylethanethioamide
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure.IC50 value:Target: AT1 receptor antagonistin vitro: Fimasartan suppressed the expressions of inducible nitric oxide synthase (iNOS) by down-regulating its transcription, and subsequently inhibited the productions of nitric oxide (NO). In addition, fimasartan attenuated LPS-induced transcriptional and DNA-binding activities of nuclear factor-kappa B (NF-κB) and

Fimasartan is a member of biphenyls.|Fimasartan is an angiotensin II receptor antagonist (ARB) drug employed in the treatment of both hypertension and heart failure. It has been found to be safe when administered with hydrochlorothiazide (a diuretic) in clinical trials. Fimasartan was initially approved September 9th, 2010 in South Korea and is marketed under the brand name Kanarb by Boryung Pharmaceuticals.

Fimasartan Basic Attributes

Molecular Weight：

501.65

Exact Mass：

501.65

UNII：

P58222188P

DSSTox ID：

DTXSID80179460

ATC Code：

C - Cardiovascular system

Characteristics

PSA：

123

XLogP3：

3.5

Density：

1.25

Boiling Point：

693.0±65.0°C at 760 mmHg

Flash Point：

372.9±34.3 °C

Refractive Index：

1.658

Drug Information

Drug Indication：

Used for the treatment of hypertension and heart failure.

Pharmacology：

Fimasartan is a selective angiotensin receptor 1 (AR1) inhibitor. It acts to lower blood pressure by inhibiting vasoconstriction

Absorption：

Tmax is 0.5-1.3 h.|Most is eliminated unchangd in bile with less than 3% in the urine.

Biological Half-Life：

The half life of elimination is 7-10 h.

Mechanism of Action：

Angiotensin II activates AR1 leading to vasoconstriction and increased noradrenaline release which further increases vasoconstriction via action at α1-adrenergic receptors. It also stimulates secretion of aldosterone which acts to increase sodium and water reabsorption in the renal tubules. Fimasartan bind to and antagonizes AR1 preventing vasoconstriction and reducing aldosterone secretion to increase natriuresis leading to a reduction in blood volume. Together these effects produce an anti-hypertensive effect.

MeSH Entry Terms：

BR-A657

Computed Properties

Molecular Weight:501.6
XLogP3:3.5
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:9
Exact Mass:501.23107981
Monoisotopic Mass:501.23107981
Topological Polar Surface Area:123
Heavy Atom Count:36
Complexity:849
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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