Home Transmembrane Transporters Calcium Channel inhibitor Felodipine For research use only.

Felodipine

Synonyms: CGH-869

Felodipine (CGH-869) is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.

Felodipine Chemical Structure

Felodipine Chemical Structure

CAS: 72509-76-3

Selleck's Felodipine has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
Click to View More Cell Line Experimental Data

Biological Activity

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.
Targets
L-type calcium channel [1]
0.15 nM
In vitro
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]
In Vivo
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 Animal Models Male Sprague-Dawley rats with approximately 5/6 renal ablation
Dosages 1 g/kg/day
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02311530 Completed Healthy Ranbaxy Laboratories Limited|Ranbaxy Inc. October 2008 Not Applicable
NCT02327247 Completed Healthy Ranbaxy Laboratories Limited|Ranbaxy Inc. September 2008 Not Applicable
NCT00392262 Completed Hypertension Novartis August 2006 Phase 3
NCT00348686 Completed Hypertension|Left Ventricular Hypertrophy AstraZeneca June 2006 Phase 4

Chemical lnformation & Solubility

Molecular Weight 384.25 Formula

C18H19Cl2NO4
CAS No. 72509-76-3 SDF Download Felodipine SDF
Smiles CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (200.39 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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