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Efonidipine HCl monoethanolate

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Chemical Structure| 111011-76-8 同义名 : 依福地平 ;NZ-105 hydrochloride monoethanolate;Efonidipine hydrochloride monoethanolate
CAS号 : 111011-76-8
货号 : A205020
分子式 : C36H45ClN3O8P
纯度 : 98%
分子量 : 714.18
MDL号 : MFCD00875717
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.