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Clevidipine Butyrate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Clevidipine Butyrate图片
CAS NO:167221-71-8
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
100mg电议

产品介绍
Clevidipine Butyrate 是一种短效二氢吡啶钙通道拮抗剂（IC50= 7.1 nM，V(H) = -40 mV），正在开发用于治疗围手术期高血压。
Cas No.167221-71-8
别名氯维地平
化学名5-O-(butanoyloxymethyl) 3-O-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
Canonical SMILESCCCC(=O)OCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
分子式C21H23Cl2NO6
分子量456.32
溶解度≥ 21.4mg/mL in DMSO
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension.IC50 Value: 7.1 nM at V(H) = -40 mV [1]Target: calcium channelin vitro: Both clevidipine and nitroglycerin completely reversed U46619-induced contraction (clevidipine (50% effective concentration [EC50] = 3.88 +/- 0.84 x 10(-6) mol/L, nitroglycerin EC50 = 4.84 +/- 2.76 x 10(-8) mol/L) [2]. A decrease in temperature increased the half-life of clevidipine in blood, whereas dilution of the blood did not affect the in vitro half-life of clevidipine. The albumin concentration affected the hydrolysis rate of clevidipine in RBC suspended with saline [3].in vivo: Clevidipine is a high-clearance drug with a relatively small volume of distribution, resulting in an extremely short half-life in all species studied. The median initial half-life of the individual value (Bayesian estimates) is 12, 20, and 22 s in the rabbit, rat, and dog, respectively [4]. The extremely high clearance value and the small volume of distribution resulted in short half-lives of clevidipine, 2.2 and 16.8 min, respectively. The blood concentration and dose rate producing half the maximal effect (i.e. EC50 and ED50) were approximately 25 nM and 1.5 microg/kg/min, respectively [5].Clinical trial: CARVE: Clevidipine for Vasoreactivity Evaluation of the Pulmonary Arterial Bed. Phase 4

References:
[1]. Yi X, Vivien B, Lynch C 3rd. Clevidipine blockade of L-type Ca2+ currents: steady-state and kinetic electrophysiological studies in guinea pigventricular myocytes.
[2]. Huraux C, Makita T, Szlam F, The vasodilator effects of clevidipine on human internal mammary artery. Anesth Analg. 1997 Nov;85(5):1000-4.
[3]. Ericsson H, et al. In vitro hydrolysis rate and protein binding of clevidipine, a new ultrashort-acting calcium antagonist metabolised by esterases, in different animal species and man. Eur J Pharm Sci. 1999 Apr;8(1):29-37.
[4]. Ericsson H, et al. Pharmacokinetics of new calcium channel antagonist clevidipine in the rat, rabbit, and dog and pharmacokinetic/pharmacodynamic relationship in anesthetized dogs. Drug Metab Dispos. 1999 May;27(5):558-64.
[5]. Schwieler JH, et al. Circulatory effects and pharmacology of clevidipine, a novel ultra short acting and vascular selective calcium antagonist, in hypertensive humans. J Cardiovasc Pharmacol. 1999 Aug;34(2):268-74.