货号	规格	价格	上海	北京	珠海	重庆	武汉
S84627-5mg买3赠1	99.90%	￥196.00 S84627-5mg ￥196.00 现货（买3赠1）	1689 >10	-	-	-	-
S84627-10mg买3赠1	99.90%	￥330.00 S84627-10mg ￥330.00 现货（买3赠1）	849 >10	-	-	-	-
S84627-50mg买3赠1	99.90%	￥799.00 S84627-50mg ￥799.00 现货（买3赠1）	176 >10	-	-	-	-
S84627-250mg买3赠1	99.90%	￥2380.00 S84627-250mg ￥2380.00 现货（买3赠1）	37 >10	-	-	-	-

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产品描述：

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). 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 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

靶点：

AT1 Receptor;Apoptosis; RAAS

体内研究：

Fimasartan (0.5 mg/kg; 口服; 33 天) 可在大鼠脑出血模型中改善 NLRP3 炎症小体介导的神经炎症和脑损伤。
Fimasartan (0.03-3 mg/kg; 口服/静脉注射; 3-24 小时) 在高血压大鼠中具有降血压作用。

参考文献：

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. Lee HW, et al. Effect of age on the pharmacokinetics of fimasartan (BR-A-657). Expert Opin Drug Metab Toxicol. 2011 Nov;7(11):1337-44. 4. Shin KH, et al. The effect of the newly developed angiotensin receptor II antagonist fimasartan on the pharmacokinetics of atorvastatin in relation to OATP1B1 in healthy male volunteers. J Cardiovasc Pharmacol. 2011 Nov;58(5):492-9.

溶解性：

DMSO : ≥ 49 mg/mL (97.68 mM)

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.993 ml	9.967 ml	19.934 ml
5 mM	0.399 ml	1.993 ml	3.987 ml
10 mM	0.199 ml	0.997 ml	1.993 ml
50 mM	0.04 ml	0.199 ml	0.399 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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Fimasartan ( BR-A-657)

2-Butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3H)-one

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)