1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
  3. Quinaprilat-d5

Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].

For research use only. We do not sell to patients.

Quinaprilat-d<sub>5</sub> Chemical Structure

Quinaprilat-d5 Chemical Structure

CAS No. : 1279034-23-9

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Description

Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].

In Vitro

Quinaprilat-d5 (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-d5 (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.

In Vivo

Quinaprilat-d5 (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].

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

Animal Model: Male spontaneous hypertensive rats (SHRs) (230-250 g)[1]
Dosage: 3 mg/kg
Administration: Oral gavage; every day; 6 days
Result: Caused a significant drop in blood pressure from day 1 to day 5 by combining quinapril and gemcabene while each alone had no effect. Decreased plasma concentration of quinaprilat on the fifth day.
Animal Model:
Dosage:
Administration:
Result: Result: The pharmacokinetic parameters of quinaprilat
Parameter
AUC(0-24 h) 4.62 μM/h
Ae(0-24 h) 23.1 μg
renal clearance 31.0 mL/h
Molecular Weight

415.49

Formula

C23H21D5N2O5

CAS No.
Unlabeled CAS

82768-85-2

Appearance

Solid

Color

White to off-white

SMILES

C([C@@H](N[C@@H](CCC1=C(C(=C(C(=C1[2H])[2H])[2H])[2H])[2H])C(O)=O)C)(=O)N2[C@H](C(O)=O)CC=3C(C2)=CC=CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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