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Lacidipine

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Chemical Structure| 103890-78-4 同义名 : GX 1048;GR-43659X;Motens;Lacimen;Lacipil;SN-305
CAS号 : 103890-78-4
货号 : A761993
分子式 : C26H33NO6
纯度 : 98%
分子量 : 455.543
MDL号 : MFCD00865936
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(109.76 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：
生物活性
靶点

  • Calcium Channel
描述 Lacidipine, a novel third-generation dihydropyridine calcium channel blocker used for hypertension. Lacidipine protects HKCs (human kidney cell) against apoptosis induced by ATP (adenosine triphosphate) depletion and recovery by regulating the caspase-3 pathway[3]. In addition to calcium channel-modulated vasodilation, lacidipine displays antioxidant activity greater than that of other dihydropyridine calcium antagonists. Lacidipine was effective in elderly patients (including those with isolated systolic hypertension), African Nigerian patients and patients with concurrent type 2 diabetes mellitus. Lower atherosclerotic progression and plaque formation with lacidipine compared with atenolol in patients completing the full 4 years of the study[4]. Lacidipine showed a significant reduction in elevated systolic blood pressure together with a great protection of ALT (alanine amine transferase) and SOD enzymes from the destructive effects of irradiation and hypertension in irradiated, hypertensive and lacidipine-treated rats[5]. Lacidipine-modified EPCs (Endothelial progenitor cells) via a partially CXCR4 (CXC chemokine receptor four) signaling contribute to enhanced endothelial repair capacity in hypertension[2]. In addition, lacidipine attenuates depression-like symptoms in reserpine-treated mice[6].
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
NCT01587742 - Completed - -
NCT00460915 Hypertension Phase 4 Completed - Korea, Republic of ... 展开 >> Korea University Guro Hospital Seoul, Korea, Republic of, 152-703 收起 <<
NCT02218684 Healthy Phase 1 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.98mL

2.20mL

1.10mL

21.95mL

4.39mL

2.20mL
参考文献

[1]Bernard E, Mialou V, et al. [Lacidipine efficacy and safety for high blood pressure treatment in pediatric oncohematology] . Arch Pediatr. 2014 Oct;21(10):1101-5.

[2]Liu X, Zhang GX, Zhang XY, et al. Lacidipine improves endothelial repair capacity of endothelial progenitor cells from patients with essential hypertension. Int J Cardiol. 2013;168(4):3317‐3326

[3]Zhang A, Fu S, Chen L, et al. Lacidipine attenuates apoptosis via a caspase-3 dependent pathway in human kidney cells. Cell Physiol Biochem. 2013;32(4):1040‐1049

[4]McCormack PL, Wagstaff AJ. Lacidipine: a review of its use in the management of hypertension. Drugs. 2003;63(21):2327‐2356

[5]Kamal SM. Possible hepatoprotective effects of lacidipine in irradiated DOCA-salt hypertensive albino rats. Pak J Biol Sci. 2013;16(21):1353‐1357

[6]Khurana K, Bansal N. Lacidipine attenuates reserpine-induced depression-like behavior and oxido-nitrosative stress in mice. Naunyn Schmiedebergs Arch Pharmacol. 2019;392(10):1265‐1275