Felodipine
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.
Purity & Quality Control
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Biological Activity
| Description | Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM. | ||||||||||||||||||||||||||||||
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| Features | Unlike many Ca2+ channel blockers, Felodipine does not have cardiac side effects due to high selectivity for vascular smooth muscle vs. myocardial tissue. | ||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
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). [1] 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. [2] 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. [3] 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. [4] 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. [5] Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM. [6] |
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| Cell Data |
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| 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. [7] 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. [8] |
Protocol
| Animal Research:[7] |
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Solubility (25°C)
| In vitro | DMSO | 77 mg/mL (200.39 mM) |
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| Ethanol | 72 mg/mL (187.37 mM) | |
| Water | Insoluble |
* 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.
Chemical Information
| Molecular Weight | 384.25 |
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| Formula | C18H19Cl2NO4 |
| CAS No. | 72509-76-3 |
| Storage | powder |
| Synonyms | CGH-869 |
Bio Calculators
Molarity Calculator
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator
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 | -- |
Tech Support
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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