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Quinaprilat

Cat. No. M25590

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Quinaprilat Structure

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Quality Control & Documentation
Biological Activity

Quinaprilat is an orally active non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin.

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 Km for quinaprilat is 13.4 μM. 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. Quinaprilat acts as anti-hypertensive agent and vasodilator.

Chemical Information
Molecular Weight 410.46
Formula C23H26N2O5
CAS Number 82768-85-2
Solubility (25°C) DMSO ≥10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Arne Georg Kieback, et al. Expert Opin Drug Metab Toxicol. Quinaprilat: a review of its pharmacokinetics, pharmacodynamics, toxicological data and clinical application

[2] Peter Korn, et al. J Thorac Cardiovasc Surg. Quinaprilat during cardioplegic arrest in the rabbit to prevent ischemia-reperfusion injury

[3] W E Haefeli, et al. Hypertension. Quinaprilat induces arterial vasodilation mediated by nitric oxide in humans

[4] E Breslin, et al. J Clin Pharmacol. A pharmacodynamic and pharmacokinetic comparison of intravenous quinaprilat and oral quinapril

[5] E J Begg, et al. Br J Clin Pharmacol. The pharmacokinetics and pharmacodynamics of quinapril and quinaprilat in renal impairment

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Keywords: Quinaprilat supplier, ACE, inhibitors, activators

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