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CAS No.: 111011-76-8

Efonidipine HCl monoethanolate/盐酸依福地平一乙醇盐 Catalog No. CSN10893

Synonyms: NZ-105 hydrochloride monoethanolate;Efonidipine HCl monoethanolate;盐酸依福地平一乙醇盐

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

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生物活性

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.4002 mL
- 7.0010 mL
- 14.0021 mL
- 5 mM
- 0.2800 mL
- 1.4002 mL
- 2.8004 mL
- 10 mM
- 0.1400 mL
- 0.7001 mL
- 1.4002 mL

技术信息

CAS号

111011-76-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C36H45ClN3O8P

运输

蓝冰

分子量

714.18

别名

NZ-105 hydrochloride monoethanolate;Efonidipine HCl monoethanolate;盐酸依福地平一乙醇盐

溶解度

DMSO	25.0 mg/mL (35.0 mM) warming
Water	Insoluble

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