Efonidipine hydrochloride monoethanolate
(Synonyms: 盐酸依福地平一乙醇盐; NZ-105 hydrochloride monoethanolate) 目录号 : GC35963
An L- and T-type calcium channel inhibitor
Cas No.:111011-76-8
Sample solution is provided at 25 µL, 10mM.
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Efonidipine is an inhibitor of L- and T-type voltage-gated calcium channels (Cavs).1 It inhibits Cav1.2a (IC50 = 1.8 nM for the hamster channel), an L-type Cav, and Cav3.2 (IC50 = 350 nM for the human channel), a T-type Cav. It also inhibits L- and T-type calcium channels and fetal bovine serum-induced hypertrophy in isolated mouse cardiomyocytes.2 Efonidipine (200 mg/kg) increases survival in a mouse model of acute myocardial infarction induced by ligation of the left coronary artery.3 Efonidipine is also an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro; IC50 = 38.5 ?M).4
1.Lee, T.-S., Kaku, T., Takebayashi, S., et al.Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca2+ channels with distinct inhibitory mechanismsPharmacology78(1)11-20(2006) 2.Horiba, M., Muto, T., Ueda, N., et al.T-type Ca2+ channel blockers prevent cardiac cell hypertrophy through an inhibition of calcineurin-NFAT3 activation as well as L-type Ca2+ channel blockersLife Sci.82(11-12)554-560(2008) 3.Kinoshita, H., Kuwahara, K., Takano, M., et al.T-type Ca2+ channel blockade prevents sudden death in mice with heart failureCirculation120(9)743-752(2009) 4.Ghahremanpour, M.M., Tirado-Rives, J., Deshmukh, M., et al.Identification of 14 known drugs as inhibitors of the main protease of SARS-CoV-2ACS Med. Chem. Lett.11(12)2526-2533(2020)
| Cas No. | 111011-76-8 | SDF | |
| 别名 | 盐酸依福地平一乙醇盐; NZ-105 hydrochloride monoethanolate | ||
| Canonical SMILES | CC1=C(P2(OCC(C)(C)CO2)=O)C(C3=CC([N+]([O-])=O)=CC=C3)C(C(OCCN(C4=CC=CC=C4)CC5=CC=CC=C5)=O)=C(C)N1.[H]Cl.CCO | ||
| 分子式 | C36H45ClN3O8P | 分子量 | 714.18 |
| 溶解度 | DMSO: 25 mg/mL (35.01 mM); Water: < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4002 mL | 7.001 mL | 14.0021 mL |
| 5 mM | 0.28 mL | 1.4002 mL | 2.8004 mL |
| 10 mM | 0.14 mL | 0.7001 mL | 1.4002 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet