Quinaprilat 

Quinaprilat is an orally active non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat acts as anti-hypertensive agent and vasodilator^[1][2].

Quinaprilat (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 K_m for Quinaprilat is 13.4 μM^[1].
Quinaprilat (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Quinaprilat (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].
The pharmacokinetic parameters of quinaprilat

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

410.46

C₂₃H₂₆N₂O₅

82768-85-2

Solid

White to off-white

O=C(O)[C@H]1N(CC2=C(C1)C=CC=C2)C([C@H](C)N[C@@H](CCC3=CC=CC=C3)C(O)=O)=O

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]