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S81998

Efonidipine hydrochloride monoethanolate

源叶(MedMol) 99%
  • 英文名:
  • Efonidipine hydrochloride monoethanolate
  • 别名:
  • 依福地平;盐酸依福地平一乙醇盐;NZ-105 hydrochloride monoethanolate
  • CAS号:
  • 111011-76-8
  • 分子式:
  • C36H45ClN3O8P
  • 分子量:
  • 714.185
  • 核磁/质谱:
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81998-5mg 99% ¥320.00元 >10 - - - EA 加入购物车
源叶(MedMol) S81998-10mg 99% ¥544.00元 >10 - - - EA 加入购物车
源叶(MedMol) S81998-50mg 99% ¥1680.00元 >10 - - - EA 加入购物车
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  • 产品描述: Efonidipine hydrochloride monoethanolate (NZ-105 hydrochloride monoethanolate) is a dual T-type and L-type calcium channel blocker (CCB). IC50 value: Target: calcium channel blocker in vitro: Efonidipine and nifedipine, but not other examined CCBs, also increased the N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP)-induced StAR mRNA, which reflects the action of adrenocorticotropic hormone, and efonidipine and R(-)-efonidipine enhanced the dbcAMP-induced DHEA-S production in NCI-H295R adrenocortical carcinoma cells. I(Ca(T)) was blocked mainly by a tonic manner by nifedipine, by a use-dependent manner by mibefradil, and by a combination of both manners by efonidipine. IC50s of these Ca2+ channel antagonists to I(Ca(T)) and L-type Ca2+ channel current (I(Ca(L))) were 1.2 micromol/l and 0.14 nmol/l for nifedipine; 0.87 and 1.4 micromol/l for mibefradil, and 0.35 micromol/l and 1.8 nmol/l for efonidipine, respectively . in vivo: Twenty hypertensive patients on chronic hemodialysis were given efonidipine 20-60 mg twice daily and amlodipine 2.5-7.5 mg once daily for 12 weeks each in a random crossover manner. The average blood pressure was comparable between the efonidipine and amlodipine periods (151 + or - 15/77 + or - 8 versus 153 + or - 15/76 + or - 8 mmHg). The pulse rate did not change significantly during the administration periods. In the UM-X7.1 group, EFO treatment significantly attenuated the decrease of LVEF without affecting blood pressure compared with the vehicle group. EFO treatment decreased heart rate (by approximately 10%) in both groups
  • 靶点: Calcium Channel;CalciumChannel
  • 参考文献:
    1. Ikeda K, et al. Efonidipine, a Ca(2+)-channel blocker, enhances the production of dehydroepiandrosterone sulfate in NCI-H295R human adrenocortical carcinoma cells. Tohoku J Exp Med. 2011;224(4):263-71. 2. Nakano N, 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. Suzuki S, et al. Beneficial effects of the dual L- and T-type Ca2+ channel blocker efonidipine on cardiomyopathic hamsters. Circ J. 2007 Dec;71(12):1970-6. 4. Lee TS, et al. Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms. Pharmacology. 2006;78(1):11-20.
  • 溶解性: DMSO  :  125  mg/mL  (175.03  mM;  Need  ultrasonic)    H2O  :  <  0.1  mg/mL  (ultrasonic;warming;heat  to  60°C)  (insoluble)
  • 保存条件: 2-8℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.4 ml 7.001 ml 14.002 ml
    5 mM 0.28 ml 1.4 ml 2.8 ml
    10 mM 0.14 ml 0.7 ml 1.4 ml
    50 mM 0.028 ml 0.14 ml 0.28 ml
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