Clevidipine Butyrate   中文名称: 丁酸氯维地平

体外：氯维地平和硝酸甘油均完全逆转U46619诱导的收缩（氯维地平（50%有效浓度[EC50] = 3.88 +/- 0.84 x 10(-6) mol/L，硝酸甘油EC50 = 4.84 +/- 2.76 x 10( -8) mol/L)。温度降低使氯维地平在血液中的半衰期增加，而血液稀释不影响氯维地平的体外半衰期。白蛋白浓度影响氯维地平在红细胞中的水解率用生理盐水悬浮

氯维地平是一种高清除率药物，分布体积相对较小，导致所有研究物种的半衰期极短。兔子、大鼠和狗的个体值初始半衰期中位数（贝叶斯估计）分别为 12、20 和 22 秒。极高的清除率和较小的分布体积导致氯维地平的半衰期较短，分别为 2.2 分钟和 16.8 分钟。产生一半最大效应（即EC50和ED50）的血液浓度和剂量率分别约为25nM和1.5μg/kg/min。

Absorption, Distribution and Excretion
urine 63-74%, feces 7-22%

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Metabolism / Metabolites
Clevidipine is rapidly hydrolyzed to inactive metabolites by esterases in arterial blood.

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Biological Half-Life
1 minute

Protein Binding
>99.5%

J Pediatr Pharmacol Ther.2015Jan-Feb;20(1):54-60.

Clevidipine is a dihydropyridine.
Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option.
Clevidipine is a Dihydropyridine Calcium Channel Blocker. The mechanism of action of clevidipine is as a Calcium Channel Antagonist.

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Drug Indication
For the reduction of blood pressure when when oral antihypertensive therapy is not feasible or not desirable.
FDA Label
Treatment of hypertensive disease

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Mechanism of Action
Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.

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Pharmacodynamics
Clevidipine belongs to a well-known class of drugs called dihydropyridine calcium channel antagonists. Clevidpine is the first third generation intravenous dihydropyridine calcium channel blocker. In vitro studies demonstrated that clevidipine acts by selectively relaxing the smooth muscle cells that line small arteries, resulting in arterial dilation, widening of the artery opening, and without reducing central venous pressure or reducing cardiac output.

C21H23CL2NO6

456.32

455.09

167221-71-8

Clevidipine-d7;(R)-Clevidipine-13C,d3

153994

White to off-white solid powder

1.3±0.1 g/cm3

539.7±50.0 °C at 760 mmHg

128-130°C

280.2±30.1 °C

0.0±1.4 mmHg at 25°C

1.543

5.46

90.93

1

7

10

30

748

0

KPBZROQVTHLCDU-UHFFFAOYSA-N

InChI=1S/C21H23Cl2NO6/c1-5-7-15(25)29-10-30-21(27)17-12(3)24-11(2)16(20(26)28-4)18(17)13-8-6-9-14(22)19(13)23/h6,8-9,18,24H,5,7,10H2,1-4H3

methyl 5-{[(butanoyloxy)methoxy]carbonyl}-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3-carboxylate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 本产品在运输和储存过程中需避光。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (5.48 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (5.48 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。