| Bioactivity | Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. | ||||||||||||
| Target | IC50: 81 μM (ACE) | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| 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 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[2]. | ||||||||||||
| Name | Zofenopril | ||||||||||||
| CAS | 81872-10-8 | ||||||||||||
| Formula | C22H23NO4S2 | ||||||||||||
| Molar Mass | 429.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |