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拉西地平 /Lacidipine {[allProObj[0].p_purity_real_show]}

货号:A761993 同义名: GX 1048;GR-43659X

Lacidipine is a L-type calcium channel blocker, used for treating high blood pressure.

Lacidipine 化学结构 CAS号:103890-78-4
Lacidipine 化学结构
CAS号:103890-78-4
Lacidipine 3D分子结构
CAS号:103890-78-4
Lacidipine 化学结构 CAS号:103890-78-4
Lacidipine 3D分子结构 CAS号:103890-78-4
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Lacidipine 纯度/质量文件 产品仅供科研

货号:A761993 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 ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

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

NCX, IC50: 33 nM

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

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 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 p38 MAPK,Akt 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。

Lacidipine 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].

Lacidipine 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 - -

Lacidipine 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

Lacidipine 实验方案

计算器
存储液制备 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

Lacidipine 技术信息

CAS号103890-78-4
分子式C26H33NO6
分子量 455.543
别名 GX 1048;GR-43659X;Motens;Lacimen;Lacipil;SN-305
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(109.76 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
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