Bioactivity | Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator[1][2]. |
Invitro | Quinaprilat hydrate (5 μM) mediates the interaction of organic anion transporter 3 (hOAT3) which can promote renal active secretion of quinapril that increases uptake of quinaprilat to 25-fold in HEK293 cells and hOAT3 affinity Km for quinaprilat is 13.4 μM[1].Quinaprilat hydrate (100 nM, 20 min) can inhibit the activity of protein kinase C (PKC) by activing the B1 receptor resulting in the release of NO in human lung microvascular endothelial (HLMVE) cells[2]. |
In Vivo | Quinaprilat hydrate (oral gavage, 3 mg/kg, every day, 6 days) has some anti-hypertensive effect by combining with other drugs in male spontaneous hypertensive rats (SHRs)[1]. Animal Model: |
Name | Quinaprilat hydrate |
CAS | 1435786-09-6 |
Formula | C23H28N2O6 |
Molar Mass | 428.48 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Haodan Yuan, et al. Renal organic anion transporter-mediated drug-drug interaction between gemcabene and quinapril. J Pharmacol Exp Ther. 2009 Jul;330(1):191-7. doi: 10.1124/jpet.108.149476. Epub 2009 Apr 6 [2]. Sinisa Stanisavljevic, et al. Angiotensin I-converting enzyme inhibitors block protein kinase C epsilon by activating bradykinin B1 receptors in human endothelial cells. J Pharmacol Exp Ther. 2006 Mar;316(3):1153-8. |