| CAS NO: | 247257-48-3 |
| 包装 | 价格(元) |
| Free Sample (0.1-0.5mg) | 电议 |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 200mg | 电议 |
| 500mg | 电议 |
| Cas No. | 247257-48-3 |
| 别名 | 非马沙坦; BR-A-657 |
| Canonical 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 |
| 分子式 | C27H31N7OS |
| 分子量 | 501.65 |
| 溶解度 | DMSO: ≥ 49 mg/mL (97.68 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 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 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 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]. [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. |
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