1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Fimasartan

Fimasartan (Synonyms: BR-A-657)

Cat. No.: HY-B0780 Purity: 98.77%
Handling Instructions

Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure.

For research use only. We do not sell to patients.

Fimasartan Chemical Structure

Fimasartan Chemical Structure

CAS No. : 247257-48-3

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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 antagonist in 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 activator protein-1 (AP-1) [1]. BR-A-657 displaced [125I][Sar1 -Ile8]angiotensin II (Ang II) from its specific binding sites to AT1 subtype receptors in membrane fractions of HEK-293 cells with an IC50 of 0.16 nM [2]. in vivo: After oral administration of 240 mg fimasartan, the mean area under the plasma concentration-time curve from time zero to infinity was 2899.0 ng/ml/h in the older, which was significantly greater than in young subjects (1767.4 ng/ml/h; p = 0.03) [3]. Compared with atorvastatin alone, coadministration of fimasartan and atorvastatin increased the atorvastatin acid mean (95% confidence interval) maximum concentration (Cmax,ss) by 1.89-fold (1.49-2.39) and the area under the concentration curve (AUCτ,ss) by 1.19-fold (0.96-1.48). Fimasartan also increased the mean 2-hydroxy atorvastatin acid Cmax,ss and AUCτ,ss by 2.45-fold (1.80-3.35) and 1.42-fold (1.09-1.85), respectively [4].

Clinical Trial
Molecular Weight

501.65

Formula

C₂₇H₃₁N₇OS

CAS No.

247257-48-3

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 49 mg/mL (97.68 mM)

*"≥" means soluble, but saturation unknown.

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Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9934 mL 9.9671 mL 19.9342 mL
5 mM 0.3987 mL 1.9934 mL 3.9868 mL
10 mM 0.1993 mL 0.9967 mL 1.9934 mL
*Please refer to the solubility information to select the appropriate solvent.
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