Fimasartan

产品编号: DC9349 Featured
Fimasartan
结构式
247257-48-3
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中国地区超过5000个高品质化合物库存
应用领域
Fimasartan(BR-A-657)是血管紧张素受体AT1非肽类拮抗剂,用于治疗高血压和心力衰竭。
Cas No.: 247257-48-3
名称:
别名: Kanarb; BR-A-657
SMILES: O=C1N(CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2)C(CCCC)=NC(C)=C1CC(N(C)C)=S
分子式: C27H31N7Os
分子量: 501.6463
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: Fimasartan(BR-A-657) is a non-peptide angiotensin II receptor antagonist used for the treatment of hypertension and heart failure. 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). 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. in vivo: After oral administration of 240 mg fimasartan, the mean area under the plasma concentration-time curve from time zero to infinity (AUC(0→∞)) 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) . 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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