For research use only.

Catalog No.S1885 Synonyms: CGH-869

2 publications

Felodipine  Chemical Structure

CAS No. 72509-76-3

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

Selleck's Felodipine has been cited by 2 publications

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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.
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 MlTtSpVv[3Srb36gZZN{[Xl? MmjyNlQhcA>? M{LmUmFkfGm4YYTpc44hd2ZicnH0JHBZWiCneIDy[ZN{\WRiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCkYYPl[EBtfW2rbnXzZ4VvfCCjbnHsfZNqeyxiRVO1NF0zOy52IN88US=> Ml\2NlA6PjZyNEO=
H9C2 cells MlT4SpVv[3Srb36gZZN{[Xl? M2HC[WlvcGmkaYTpc44hd2ZiTD3WSGNEKGmwIILheEBJQUN{IHPlcIx{KGG|c3Xzd4VlKGG|IHXm[oVkfCCxbjDjZYxkcXWvIHzleoVtKGK7IF\seY8uPCCobIXvdoV{[2WwY3WgZZN{[Xl? MVWxPVg5ODN{Mx?=
HepG2 (DPX-2) cells Ml;0SpVv[3Srb36gZZN{[Xl? M1\FT|I1KGh? NE\WUJRC[3SrdnH0bY9vKG:oIHj1cYFvKFC[UjDlfJBz\XO|ZXSgbY4hcHWvYX6gTIVxTzJiKFTQXE0zMSClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gR3lRO0F2IHHmeIVzKDJ2IHjyd{BjgSCudX3pcoV{[2WwdDDhcoFtgXOrczygSWM2OD1zLkmg{txO NIPLfpkzODl4NkC0Ny=>

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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]


Animal Research:[7]
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  • Animal Models: Male Sprague-Dawley rats with approximately 5/6 renal ablation
  • 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
Smiles CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID