Eprosartan|133040-01-4|(SKF-108566J free base)-陌孚医药/Medlife

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Eprosartan (Synonyms: SKF-108566J free base)

目录号: PL14748 纯度: ≥95%

CAS No. :133040-01-4

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中文名称	Eprosartan
中文别名	依普罗沙坦;依普沙坦;(E)- Α-[[2-丁基-1-[(4-羧基苯基)甲基]-1H-咪唑-5-基]亚甲基]-2-噻吩丙酸;N-苄氧羰基-DL-色氨酸;普沙坦-D4;依普罗沙坦杂质;甲磺酸依普沙坦;依普沙坦-D4;EPROSARTAN 醋酸盐形式
英文名称	Eprosartan
英文别名	Eprosartan;Eprosartan Mysylate;(E)-3-[2-Butyl-1-[(4-carboxyphenyl)-methyl]imidazol-5-l]-2-(2-thienylmethyl)-2-propenoic Acid;((E)-3-[2-Butyl-1-[(4-carboxyphenyl)methyl]imidazol-5-yl]-2-(2-thienylmethyl)-2-propenoic Acid;(E)- α-[[2-Butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-y1]methylene]2-thiophenepropanoic acid;SKF-108566J;Teveten;Eporlosartan;(E)-4-((2-Butyl-5-(2-carboxy-3-(thiophen-2-yl)prop-1-en-1-yl)-1H-imidazol-1-yl)methyl)benzoic acid;Des[2-(2-thienylMethyl)] Eprosartan-2-carboxylic Acid;Eprosartan-d9;4-[[2-butyl-5-[(E)-2-carboxy-3-thiophen-2-ylprop-1-enyl]imidazol-1-yl]methyl]benzoic acid;(E)-3-[2-Butyl-1-[(4-carboxyphenyl)methyl]imidazol-5-yl]-2-(2-thienylmethyl)-2-propenoic acid;Navixen;SKB 108566;Eprosartan-d4;SKF-108566);prop-1-en-1-yl);-1H-imidazol-1-yl)
Cas No.	133040-01-4
分子式	C₂₃H₂₄N₂O₄S
分子量	424.51
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months

产品详情

Eprosartan (SKF-108566J free base) 是一种选择性，竞争性，非肽和具有口服活性的血管紧张素 II 受体 (angiotensin II receptor) 拮抗剂，可用作降压剂。Eprosartan 结合血管紧张素 II 受体，在大鼠和人类肾上腺皮质膜中的 IC₅₀ 值分别为 9.2 nM 和 3.9 nM。

生物活性

Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC 50 s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .

性状

Solid

体外研究(In Vitro)

Eprosartan (SKF-108566J) inhibits [I]AII binding to human liver membranes (IC50 of 1.7 nM) and to rat mesenteric artery membranes (IC50 of 1.5 nM). In rabbit aortic smooth muscle cells, Eprosartan caused a concentration-dependent inhibition of AII-induced increases in intracellular Ca levels. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In conscious normotensive rats, i.v. administration of Eprosartan (0.01-0.3 mg/kg) produced dose-dependent parallel shifts in the AII pressor dose-response curve. Administration of Eprosartan (3-10 mg/kg) intraduodenally or intragastrically to conscious normotensive rats resulted in a dose-dependent inhibition of the pressor response to AII (250 ng/kg, i.v.). At 10 mg/kg, i.d., significant inhibition of the pressor response to AII was observed for 3 hr. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；In solvent -80°C 6 months

ClinicalTrial

参考文献

[1]. R M Edwards, et al. Pharmacological characterization of the nonpeptide angiotensin II receptor antagonist, SK&F 108566. J Pharmacol Exp Ther. 1992 Jan;260(1):175-81.

溶解度数据	In Vitro: DMSO : 125 mg/mL (294.46 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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