Fimasartan

Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1[1][2][3].

Product Specifications

CAS Number

[247257-48-3]

Product Name Alternative

BR-A-657

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Angiotensin Receptor; Apoptosis; NF-κB

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Endocrinology; Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Fimasartan.html

Purity

99.60

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C(CCCC)=NC(C)=C1CC(N(C)C)=S)CC2=CC=C(C3=C(C4=NN=NN4)C=CC=C3)C=C2

Molecular Formula

C27H31N7OS

Molecular Weight

501.65

Precautions

H302, H315, H319, H335

References & Citations

[1]Ryu S, et al. Fimasartan, anti-hypertension drug, suppressed inducible nitric oxide synthase expressions via nuclear factor-kappa B and activator protein-1 inactivation. Biol Pharm Bull. 2013;36 (3) :467-74.|[2]Chi YH, et al. Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist. Biol Pharm Bull. 2013;36 (7) :1208-15.|[3]Yang X, Sun J, Kim TJ, Kim YJ, Ko SB, Kim CK, Jia X, Yoon BW. Pretreatment with low-dose fimasartan ameliorates NLRP3 inflammasome-mediated neuroinflammation and brain injury after intracerebral hemorrhage. Exp Neurol. 2018 Dec;310:22-32.