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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > EfonidipineCAS：111011-63-3
Molecular Formula：C34H38N3O7P
Molecular Weight：631.66
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Off-white to light yellow Solid
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| CAS | 111011-63-3 |
| Name | Efonidipine |
| Molecular Formula | C34H38N3O7P |
| Molecular Weight | 631.66 |
| Solubility | Soluble in DMSO(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Off-white to light yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00865899 |
| SMILES | CC1=C(C(C(=C(N1)C)P2(=O)OCC(CO2)(C)C)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OCCN(CC4=CC=CC=C4)C5=CC=CC=C5 |
| InChIKey | NSVFSAJIGAJDMR-UHFFFAOYSA-N |
| InChI | InChI=1S/C34H38N3O7P/c1-24-30(33(38)42-19-18-36(28-15-9-6-10-16-28)21-26-12-7-5-8-13-26)31(27-14-11-17-29(20-27)37(39)40)32(25(2)35-24)45(41)43-22-34(3，4)23-44-45/h5-17，20，31，35H，18-19，21-23H2，1-4H3 |
| PubChem CID | 119171 |
| Target Point | Calcium Channel |
| Passage | Membrane Transporter&Ion Channel |
| Background | Efonidipine is an L - and T-type calcium channel blocker that causes vasodilation and decreased cardiac automaticity. |
| Biological Activity | Efonidipine 是一种L型和T型钙离子通道阻滞剂，可引起血管舒张和心脏自律性降低。能抑制醛固酮从肾上腺分泌。[1-2] |
| In Vitro | 依福地平对人肾上腺皮质细胞系(H295R)中醛固酮的合成和分泌具有抑制作用，这种作用至少部分是通过抑制 11-β- 羟化酶和醛固酮合成酶的表达来实现的。依福地平还能抑制 Ang II 和 K+诱导的醛固酮分泌，但它阻断后者的浓度远低于前者。[2] |
| In Vivo | 使用 LTCC、TTCC、DMT1 阻断剂和 DFO 治疗可减少铁超载地中海贫血小鼠的心脏铁沉积、心脏丙二醛(MDA)和血浆非转铁蛋白结合铁，并改善心率变异性和左心室(LV)功能。只有 TTCC 和 DMT1 阻断剂以及 DFO 能减少铁超载地中海贫血小鼠的肝脏铁积累、肝脏 MDA 和血浆 MDA，并降低死亡率。[1] |
| Cell Experiment | 将H295R细胞以0.2 × 106的密度在6孔板中孵育48小时，然后用含有0.2% UltroserSF的低血清培养基替换培养基，然后用Ang II(100 nmol/L)或KCl(10 mmol/L)(含或不含指示浓度的Ca2+通道阻滞剂)处理细胞24小时。然后收集细胞，并使用异硫氰酸-苯酚氯仿法提取细胞总RNA。根据260 nm吸光度定量提取的RNA后，500ng等量逆转录。[2] |
| Animal Experiment | 通过给基因改变的β-地中海贫血小鼠和成年野生型小鼠喂食铁饮食(0.2%二茂铁w/w)3个月，诱导它们出现铁过载情况。 然后，在连续喂食铁的同时给予 LTCC(维拉帕米和硝苯地平)、TTCC(依福地平)和 DMT1(依布硒)阻断剂以及铁螯合剂去铁胺(DFO)1 个月。[1] |
| Data Literature Source | [1]. Kumfu S，et al. T-type calcium channel blockade improves survival and cardiovascular function in thalassemic mice. Eur J Haematol. 2012 Jun;88(6): 535-48. [2]. Imagawa K，et al. Inhibitory effect of efonidipine on aldosterone synthesis and secretion in human adrenocarcinoma (H295R) cells. J Cardiovasc Pharmacol. 2006 Jan;47(1): 133-8. |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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