Quinaprilat-d₅  (Synonyms: 喹那普利-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].

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 K_m 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].

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

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].

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
分子量	415.49
Formula	C23H21D5N2O5
CAS 号	1279034-23-9
性状	固体
颜色	White to off-white
中文名称	喹那普利-d5
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
纯度 & 产品资料	Data Sheet (535 KB) SDS (252 KB) 产品使用指南 (1538 KB)
参考文献	[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.  [Content Brief] [3]. Kieback AG, et al. Quinaprilat: a review of its pharmacokinetics, pharmacodynamics, toxicological data and clinical application. Expert Opin Drug Metab Toxicol. 2009;5(10):1337-1347.  [Content Brief]

• [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.

  [3]. Kieback AG, et al. Quinaprilat: a review of its pharmacokinetics, pharmacodynamics, toxicological data and clinical application. Expert Opin Drug Metab Toxicol. 2009;5(10):1337-1347.

Quinaprilat-d₅ 相关分类

• Metabolic Enzyme/Protease
• Angiotensin-converting Enzyme (ACE)

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
kg g mg μg ng pg	=	M mM μM nM pM	×	L mL μL	×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 (start)	×	体积 (start)	=	浓度 (final)	×	体积 (final)
M mM μM nM pM	×	L mL μL	=	M mM μM nM pM	×	L mL μL
C1		V1		C2		V2

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Keywords:

Quinaprilat-d₅1279034-23-9喹那普利-d₅Angiotensin-converting Enzyme (ACE)metabolitedeuteriumisotopevasodilatorangiotensinInhibitorinhibitorinhibit

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