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丁酸氯维地平 /Clevidipine {[allProObj[0].p_purity_real_show]}

货号:A387256 同义名: 氯维地平 / rac-Clevidipine;Clevidipine Butyrate

Clevidipine is a short-acting dihydropyridine calcium channel antagonist with IC50 of 7.1 nM, it's under development for treatment of perioperative hypertension.

Clevidipine 化学结构 CAS号:167221-71-8
Clevidipine 化学结构
CAS号:167221-71-8
Clevidipine 3D分子结构
CAS号:167221-71-8
Clevidipine 化学结构 CAS号:167221-71-8
Clevidipine 3D分子结构 CAS号:167221-71-8
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Clevidipine 纯度/质量文件 产品仅供科研

货号:A387256 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

ERK,ROS,p38 MAPK 99%+
Fasudil HCl Rho,PKA 98%
ML-9 Akt,MLCK 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 98%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 98%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 98%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 98%
Cinepazide Maleate 98%
Terfenadine 98%
YM-58483 99%+
Ranolazine 98%
Praeruptorin A Akt,p38 MAPK 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Clevidipine 生物活性

靶点
  • Calcium Channel

描述 Clevidipine is a short-acting dihydropyridine calcium channel antagonist. Clevidipine is an ultrashort-acting drug for rapid reduction of blood pressure by selectively acting on the L-type Ca2+ channels on arteriolar smooth muscle. The drug's ultrashort action in reducing the blood pressure is due to its rapid hydrolysis by blood and extravascular tissue esterases, which does not depend on hepato-renal metabolism and excretion[3]. When myocytes were voltage-clamped with holding potential (VH) at -80 mV, 10 nM clevidipine decreased ICa at 0 mV by approximately 30%, but >50% when VH was -40 mV[4]. Clevidipine is an endothelium-independent arterial vasodilator that offers a potential therapeutic option in the treatment of perioperative arterial graft vasospasm and/or hypertension[2]. Clevidipine provided rapid BP control in patients with acute neurological injuries (including intracerebral haemorrhage, subarachnoid haemorrhage and acute ischaemic stroke), and was not associated with 'overshoot' in the vast majority of patients. Intravenous clevidipine was generally well tolerated and was usually associated with no reflex tachycardia or only very modest increases in heart rate[5]. Clevidipine administration during initial medical management of aortic dissection showed similar efficacy compared to SNP (sodium nitroprusside) when used as adjunct therapy to esmolol[6].

Clevidipine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01369147 Critical Illness Phase 2 Suspended(The study has been h... 展开 >>alted pending additional funding.) 收起 << October 2019 United States, Georgia ... 展开 >> Emory University Hospital Atlanta, Georgia, United States, 30322 收起 <<
NCT03719001 Vascular Diseases Early Phase 1 Recruiting October 1, 2020 United States, California ... 展开 >> University of California San Francisco Recruiting San Francisco, California, United States, 94122 Contact: Pekka Talke, MD    415-476-8963    pekka.talke@ucsf.edu    Contact: Pekka Talke, MD    415-476-8963    talkep@anesthesia.ucsf.edu 收起 <<
NCT01033370 Aortic Aneurysm ... 展开 >> Aortic Disease 收起 << Phase 4 Terminated(Project lacked fund... 展开 >>ing.) 收起 << - United States, Texas ... 展开 >> The Methodist Hospital Houston, Texas, United States, 77030 收起 <<

Clevidipine 参考文献

[1]Ericsson H, Tholander B, 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.

[2]Huraux C, Makita T, Szlam F, Nordlander M, Levy JH. The vasodilator effects of clevidipine on human internal mammary artery. Anesth Analg. 1997;85(5):1000‐1004

[3]Espinosa A, Ripollés-Melchor J, Casans-Francés R, et al. Perioperative Use of Clevidipine: A Systematic Review and Meta-Analysis. PLoS One. 2016; 11(3):e0150625. Published 2016 Mar 28

[4]Yi X, Vivien B, Lynch C 3rd. Clevidipine blockade of L-type Ca2+ currents: steady-state and kinetic electrophysiological studies in guinea pig ventricular myocytes. J Cardiovasc Pharmacol. 2000; 36(5):592‐600

[5]Keating GM. Clevidipine: a review of its use for managing blood pressure in perioperative and intensive care settings. Drugs. 2014;74(16):1947‐1960

[6]Ulici A, Jancik J, Lam TS, Reidt S, Calcaterra D, Cole JB. Clevidipine versus sodium nitroprusside in acute aortic dissection: A retrospective chart review. Am J Emerg Med. 2017; 35(10):1514‐1518

Clevidipine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.96mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL

Clevidipine 技术信息

CAS号167221-71-8
分子式C21H23Cl2NO6
分子量 456.316
别名 氯维地平 ;rac-Clevidipine;Clevidipine Butyrate;Clevelox;167221-71-8;Cleviprex
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 50 mg/mL(109.57 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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