Zofenopril
目录号: PL14779
CAS No. :81872-10-8
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中文名称
Zofenopril
中文别名
佐芬普利;(4S)-3-(苯甲酰硫基)-2(S)-甲基丙酰-4-(苯硫基)-L-脯氨酸;1-萘乙酸;佐芬普利-D5(苯甲酸-D5);佐芬普利-D5(噻吩-D5);佐芬普利钙;左芬普利
英文名称
Zofenopril
英文别名
zofenopril;(4s)-n-[3-(benzoylsulfanyl)-2(s)-methylpropionyl]-4-(phenylsulfanyl)-l-proline;(2S,4S)-1-[(2S)-3-benzoylsulfanyl-2-methylpropanoyl]-4-phenylsulfanylpyrrolidine-2-carboxylic acid;L-Proline, 1-[(2S)-3-(benzoylthio)-2-methyl-1-oxopropyl]-4-(phenylthio)-,(4S)-;1-NAPHTHALENEACETIC ACID;UNII-290ZY759PI;Zofenoprilum;Zoprace;Zofenopril
Cas No.
81872-10-8
分子式
C22H23NO4S2
分子量
429.55
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Zofenopril 是一个 angiotensin-converting enzyme (ACE) 抑制剂,其 IC50 值为 81 μM。
生物活性
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC 50 of 81 μM.
性状
Solid
IC50 & Target[1][2]
IC50: 81 μM (ACE)
体外研究(In Vitro)
Kinetic analyses demonstrate that enalapril inhibits the uptake of GlySar in a competitive manner (Ki approximately 6 mM). Fosinopril and Zofenopril have the greatest inhibitory potency (IC50 values of 55 and 81μM, respectively) while the other ACE inhibitors exhibit low-affinity interactions with the renal peptide transporter. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Zofenopril, a sulphydrylic compound, at doses higher than 70 mg/kg i.p. produces significant protection (i.e. at 70 mg/kg, P=0.044, F=2.17, d.f.=18; at higher concentration P<0.05) against the tonic phase of the audiogenic seizure response. Pretreatment with Zofenopril (15 mg/kg, i.p.) is able to produce a consistent shift to the left of the dose-response curves and a significant reduction of ED 50 values against clonus of some AEDs with the exceptions of diazepam, felbamate, phenobarbital and phenytoin compare with concurrent groups, suggesting an increase in anticonvulsant activity. 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;4°C 2 years
ClinicalTrial
参考文献
[1]. Lin CJ, et al. Competitive inhibition of glycylsarcosine transport by enalapril in rabbit renal brush border membrane vesicles: interaction of ACE inhibitors with high-affinity H+/peptide symporter. Pharm Res. 1999 May;16(5):609-15.
[2]. Sarro GD, et al. Fosinopril and zofenopril, two angiotensin-converting enzyme (ACE) inhibitors, potentiate the anticonvulsant activity of antiepileptic drugs against audiogenic seizures in DBA/2 mice. Pharmacol Res. 2012 Mar;65(3):285-96.
溶解度数据
In Vitro: DMSO : 5 mg/mL (11.64 mM; Need ultrasonic)配制储备液
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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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