Catalog No.S1885 Synonyms: CGH-869

Felodipine  Chemical Structure

Molecular Weight(MW): 384.25

Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.

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In DMSO USD 130 In stock
USD 310 In stock
USD 670 In stock
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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.
L-type calcium channel [1]
0.15 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells NEixdnpHfW6ldHnvckBie3OjeR?= NFPNdZQzPCCq MlPZRYN1cX[jdHnvckBw\iC{YYSgVHhTKGW6cILld5Nm\CCrbjDoeY1idiCKZYDHNkBk\WyuczDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGKjc3XkJIx2dWmwZYPj[Y51KGGwYXz5d4l{NCCHQ{WwQVI{NjRizszN MnfaNlA6PjZyNEO=
H9C2 cells MXHGeY5kfGmxbjDhd5NigQ>? M4XTeWlvcGmkaYTpc44hd2ZiTD3WSGNEKGmwIILheEBJQUN{IHPlcIx{KGG|c3Xzd4VlKGG|IHXm[oVkfCCxbjDjZYxkcXWvIHzleoVtKGK7IF\seY8uPCCobIXvdoV{[2WwY3WgZZN{[Xl? M{jTOlE6QDhyM{Kz
HepG2 (DPX-2) cells NEexc2hHfW6ldHnvckBie3OjeR?= NFT1ZpEzPCCq MoPtRYN1cX[jdHnvckBw\iCqdX3hckBRYFJiZYjwdoV{e2WmIHnuJIh2dWGwIFjldGczKCiGUGitNkkh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIFPZVFNCPCCjZoTldkAzPCCqcoOgZpkhdHWvaX7ld4NmdnRiYX7hcJl{cXNuIFXDOVA:OS57IN88US=> M4DGfFIxQTZ4MESz

... Click to View More Cell Line Experimental Data

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]


Animal Research:[7]
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  • Animal Models: Male Sprague-Dawley rats with approximately 5/6 renal ablation
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: 1 g/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (200.39 mM)
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


CAS No. 72509-76-3
Storage powder
in solvent
Synonyms CGH-869

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID