产品说明书

Felodipine

Print
Chemical Structure| 72509-76-3 同义名 : H 154/82;CGH-869;Felodipine, Agon, Felo-Puren, Felobeta, Felocor, Felodipin, Felodur Felogamma, Fensel, Flodil, Modip, Munobal, Perfudal, Plendil, Renedil
CAS号 : 72509-76-3
货号 : A268185
分子式 : C18H19Cl2NO4
纯度 : 98%
分子量 : 384.254
MDL号 : MFCD00868316
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(273.26 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

    L-type calcium channel, IC50:0.15 nM
描述 Felodipine is a long-acting 1,4-dihydropyridine calcium channel blocker. Felodipine significantly relaxes KCl-contracted porcine coronary segments by blocking the Ca2+ channels, displaying ~50 times more potent than nifedipine (IC50 of ~8 nM) and ~430 times than verapamil (IC50 of ~65 nM) [3]. Felodipine significantly induces the transcription and secretion of IL-6 and IL-8 with ED50 values of 5.8 nM and 5.3 nM in primary human VSMC and lung fibroblasts, respectively, while propranolol or furosemide fails to affect the expression of the two IL genes[4]. Felodipine blocks the muscarinic receptor-mediated (carbachol) Ca2+-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM[5]. In hypertensive patients, felodipine does not appear to significantly affect glomerular filtration rate, creatinine clearance, glucose tolerance, or plasma lipoprotein concentrations. In the management of hypertension, felodipine 5-40 mg/d significantly reduces systolic and diastolic BP. Adverse effects associated with felodipine are similar to those of other dihydropyridine calcium-channel antagonists and include peripheral edema, headache, dizziness, flushing, and fatigue. Felodipine appears to be safe and effective for the management of hypertension when used alone or in combination with other antihypertensive agents[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
H9C2 cells Function assay Inhibition of L-VDCC in rat H9C2 cells assessed as effect on calcium level by Fluo-4 fluorescence assay 19880323
HepG2 (DPX-2) cells Function assay 24 h Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=1.9 μM 20966043
HepG2 cells Function assay 24 h Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50=23.4 μM 20966043
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

13.01mL

2.60mL

1.30mL

26.02mL

5.20mL

2.60mL
参考文献

[1]Yiu S, Knaus EE. Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem. 1996 Nov 8;39(23):4576-82.

[2]Rodler S, Roth M, Nauck M, et al. Ca(2+)-channel blockers modulate the expression of interleukin-6 and interleukin-8 genes in human vascular smooth muscle cells. J Mol Cell Cardiol. 1995 Oct;27(10):2295-302.

[3]Johnson JD, Fugman DA. Calcium and calmodulin antagonists binding to calmodulin and relaxation of coronary segments. J Pharmacol Exp Ther. 1983;226(2):330‐334

[4]Rödler S, Roth M, Nauck M, Tamm M, Block LH. Ca(2+)-channel blockers modulate the expression of interleukin-6 and interleukin-8 genes in human vascular smooth muscle cells. J Mol Cell Cardiol. 1995;27(10):2295‐2302

[5]Yiu S, Knaus EE. Synthesis, biological evaluation, calcium channel antagonist activity, and anticonvulsant activity of felodipine coupled to a dihydropyridine-pyridinium salt redox chemical delivery system. J Med Chem. 1996;39(23):4576‐4582

[6]Yedinak KC, Lopez LM. Felodipine: a new dihydropyridine calcium-channel antagonist. DICP. 1991;25(11):1193‐1206