Zofenopril
产品编号:Bellancom-108321| CAS NO:81872-10-8| 分子式:C22H23NO4S2| 分子量:429.55
Zofenopril 是一个 angiotensin-converting enzyme (ACE) 抑制剂,其 IC50 值为 81 μM。
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Zofenopril
产品介绍 | Zofenopril 是一个 angiotensin-converting enzyme (ACE) 抑制剂,其 IC50 值为 81 μM。 | ||||||||||||||||
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生物活性 | Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. | ||||||||||||||||
体外研究 |
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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 |
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 ED50 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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 |
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 ED50 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. 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 5 mg/mL (11.64 mM; Need ultrasonic) 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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参考文献 |
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危害码 (欧洲) | Xn: Harmful;Xi: Irritant; |
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风险声明 (欧洲) | R22 |
安全声明 (欧洲) | 23-24/25 |
WGK德国 | 3 |
RTECS号 | QJ0875000 |
~% ![]() 81872-10-8 |
文献:Tetrahedron Letters, , vol. 52, # 13 p. 1493 - 1494 |
~% ![]() 81872-10-8 |
文献:WO2010/84515 A2, ; Page/Page column 33 ; |
~% ![]() 81872-10-8 |
文献:WO2010/84515 A2, ; Page/Page column 32 ; |
~74% ![]() 81872-10-8 |
文献:Krapcho; Turk; Cushman; Powell; DeForrest; Spitzmiller; Karanewsky; Duggan; Rovnvak; Schwartz; Natarajan; Godfrey; Ryono; Neubeck; Atwa; Petrillo Jr. Journal of Medicinal Chemistry, 1988 , vol. 31, # 6 p. 1148 - 1160 |
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