For research use only.
Catalog No.S1885 Synonyms: CGH-869
CAS No. 72509-76-3
Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.
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Choose Selective Calcium Channel Inhibitors
|Description||Felodipine (CGH-869) 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)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02311530||Completed||Drug: Felodipine|Drug: Felodipine (Plendil®)||Healthy||Ranbaxy Laboratories Limited|Ranbaxy Inc.||October 2008||Not Applicable|
|NCT02327247||Completed||Drug: Felodipine|Drug: PLENDIL®||Healthy||Ranbaxy Laboratories Limited|Ranbaxy Inc.||September 2008||Not Applicable|
|NCT00392262||Completed||Drug: valsartan + amlodipine||Hypertension||Novartis||August 2006||Phase 3|
|NCT00348686||Completed||Drug: Candesartan|Drug: Felodipine||Hypertension|Left Ventricular Hypertrophy||AstraZeneca||June 2006||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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