Catalog No.S1885 Synonyms: CGH-869
Molecular Weight(MW): 384.25
Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.|
|Features||Unlike many Ca2+ channel blockers, Felodipine does not have cardiac side effects due to high selectivity for vascular smooth muscle vs. myocardial tissue.|
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).  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.  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.  Felodipine at low concentration of 0.1 μM is sufficient to increases NOx generation, Ca2+-dependent NOS activity, and eNOS protein mass in rat endothelial cells.  Felodipine (10 μM) reduces nuclear translocation of p42/44 mitogen-activated protein kinase and Elk-1 activation stimulated by PDGF-BB, leading to the inhibition of human SMC proliferation.  Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM. 
|In vivo||Oral administration of Felodipine significantly reduces the average blood pressure (BP) in rats with 5/6 renal ablation, but causes additional impairment of the already impaired renal autoregulation.  Administration of Felodipine significantly reduces systolic blood pressure (SBP), serum insulin, intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by blocking NF-κB activation, and decreases macrophages in the aortic wall, leading to the modulation of vascular inflammatory response. |
-  Johnson JD, et al. J Pharmacol Exp Ther, 1983, 226(2), 330-334.
-  R?dler S, et al. J Mol Cell Cardiol, 1995, 27(10), 2295-2302.
-  Yiu S, et al. J Med Chem, 1996, 39(23), 4576-4582.
|In vitro||DMSO||77 mg/mL (200.39 mM)|
|Ethanol||72 mg/mL (187.37 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02744872||Completed||Disorder Related to Lung Transplantation||Rigshospitalet, Denmark||September 2013||Phase 4|
|NCT02232269||Completed||Food-Drug Interactions||Lawson Health Research Institute||February 2012||Phase 1|
|NCT01520285||Completed||Hypertension||Lees Pharmaceutical Limited||December 2011||Phase 4|
|NCT00841880||Completed||Hypertension||Sanofi||January 2009||Phase 4|
|NCT00905333||Completed||Healthy||AstraZeneca|Scentryphar Clinical Research|Cori Analyticals|Clínica São Lucas, Hospital Sírio Libanês de Itatiba S/C|LabClin Laboratório Clínico|Laboratório de Patologia Clínica Dr. Franceschi Ltda.|Faculdade de Ciências Farmacêuticas de Ribeirão Preto - Centro de Bioequivalência||October 2008||Phase 1|
|NCT02311530||Completed||Healthy||Ranbaxy Laboratories Limited|Ranbaxy Inc.||October 2008||--|
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