Fosinopril

Fosinopril (SQ28555) is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value of 0.18 μM[1]. Fosinopril demonstrates a non-competitive inhibition effect on ACE activity with a Ki value of 1.675 μM[2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Angiotensin-converting Enzyme (ACE)

IC50: 0.18 μM; Ki: 1.675 μM

Fosinopril (0, 1, 10, 33, 100μM; 30 min) partially inhibits the cosedimentation of liposomes and recombinant LPLA2[1]. Fosinopril (250 nM) shows no inhibition of the soluble esterase activity of LPLA2[1]. Fosinopril (0.372, 0.744, 1.116 μM) displays a non-competitive inhibition effect on ACE activity with a Ki value of 1.675 μM[2].

Fosinopril (orally; 4.67 mg/kg; 4 weeks) downregulates the creatine kinase (CK) and lactate dehydrogenase (LDH) levels and against cardiac dysfunction and structural alteration[3]. Fosinopril (orally; 4.67 mg/kg; 4 weeks) suppresses cleaved-caspase 3 expression and myocardial apoptosis in AMI rat model[3]. Animal Model: HF post-acute myocardial infarction (AMI) rat model (SPF-grade Sprague-Dawley (SD) rats, 265 ± 15 g) [3] Dosage: 4.67 mg/kg Administration: p.o.; 4 weeks Result: Against cardiac dysfunction and structural alteration and suppressed apoptosis.

[1]. Ondetti, M.A., Structural relationships of angiotensin converting-enzyme inhibitors to pharmacologic activity. Circulation, 1988. 77(6 Pt 2): p. I74-8.

[2]. Piepho, R.W., Overview of the angiotensin-converting-enzyme inhibitors. Am J Health Syst Pharm, 2000. 57 Suppl 1: p. S3-7.

[3]. Sharma, S., et al., The hemodynamic effects of long-term ACE inhibition with fosinopril in patients with heart failure. Fosinopril Hemodynamics Study Group. Am J Ther, 1999. 6(4): p. 181-9.