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盐酸依福地平一乙醇盐 /Efonidipine HCl monoethanolate {[allProObj[0].p_purity_real_show]}

货号:A205020 同义名: 依福地平 / NZ-105 hydrochloride monoethanolate;Efonidipine hydrochloride monoethanolate

Efonidipine HCl monoethanolate is a dual T-type and L-type calcium channel blocker (CCB).

Efonidipine HCl monoethanolate 化学结构 CAS号:111011-76-8
Efonidipine HCl monoethanolate 化学结构
CAS号:111011-76-8
Efonidipine HCl monoethanolate 3D分子结构
CAS号:111011-76-8
Efonidipine HCl monoethanolate 化学结构 CAS号:111011-76-8
Efonidipine HCl monoethanolate 3D分子结构 CAS号:111011-76-8
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Efonidipine HCl monoethanolate 纯度/质量文件 产品仅供科研

货号:A205020 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。

Efonidipine HCl monoethanolate 生物活性

靶点
  • Calcium Channel

描述 Efonidipine Hydrochloride Monoethanolate, a L- and T-type dual calcium channel blocker, is suggested to have a heart rate (HR)-slowing action in addition to a blood pressure (BP)-lowering effect with IC50s of 0.35 mM and 1.8 nM for I(Ca(T)) and L-type Ca2+ channel current (I(Ca(L))), respectively[3]. In vivo research confirmed that efonidipine hydrochloride monoethanolate (40-60 mg) treatment significantly reduced the HR by 11.9% in patients with mild-to-moderate essential hypertension. Efonidipine hydrochloride monoethanolate also decreased the trough systolic and diastolic BP by 11.7 and 8.6 mmHg, respectively. Efonidipine hydrochloride monoethanolate was well-tolerated[3]. Studies showed that efonidipine hydrochloride monoethanolate prevents the sudden death and arrhythmogenicity otherwise seen in dnNRSF-Tg mice[4].

Efonidipine HCl monoethanolate 参考文献

[1]Ikeda K, Saito T, Tojo K. Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011 Aug;224(4):263-71.

[2]Nakano N, Ishimitsu T, et al.Effects of efonidipine, an L- and T-type calcium channel blocker, on the renin-angiotensin-aldosterone system in chronic hemodialysis patients. Int Heart J. 2010 May;51(3):188-92.

[3]Oh IY, Seo MK, Lee HY, Kim SG, Kim KS, Kim WH, Hyon MS, Han KR, Lim SJ, Kim CH. Beneficial Effect of Efonidipine, an L- and T-Type Dual Calcium Channel Blocker, on Heart Rate and Blood Pressure in Patients With Mild-to-Moderate Essential Hypertension. Korean Circ J. 2010 Oct;40(10):514-9. doi: 10.4070/kcj.2010.40.10.514. Epub 2010 Oct 31. PMID: 21088755; PMCID: PMC2978294.

[4]Kinoshita H, Kuwahara K, Takano M, Arai Y, Kuwabara Y, Yasuno S, Nakagawa Y, Nakanishi M, Harada M, Fujiwara M, Murakami M, Ueshima K, Nakao K. T-type Ca2+ channel blockade prevents sudden death in mice with heart failure. Circulation. 2009 Sep 1;120(9):743-52. doi: 10.1161/CIRCULATIONAHA.109.857011. Epub 2009 Aug 17. PMID: 19687356.

Efonidipine HCl monoethanolate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.40mL

0.28mL

0.14mL

7.00mL

1.40mL

0.70mL

14.00mL

2.80mL

1.40mL

Efonidipine HCl monoethanolate 技术信息

CAS号111011-76-8
分子式C36H45ClN3O8P
分子量 714.18
别名 依福地平 ;NZ-105 hydrochloride monoethanolate;Efonidipine hydrochloride monoethanolate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 120 mg/mL(168.02 mM),配合低频超声助溶,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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