Felodipine

Catalog No.S1885

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
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Felodipine  Chemical Structure

Felodipine Chemical Structure
Molecular Weight: 384.25

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Felodipine is a selective L-type Ca2+ channel blocker with IC50 of 0.15 nM.
Targets L-type calcium�channel [1]
IC50 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]
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]
Features Unlike many Ca2+ channel blockers, Felodipine does not have cardiac side effects due to high selectivity for vascular smooth muscle vs. myocardial tissue.

Protocol(Only for Reference)

Kinase Assay: [1]

The effect of Felodipine on tension in coronary segments The cylindrical coronary segments from porcine hearts are inverted and fixed horizontally between a stationary bottom pin and a top pin connected to the lever of a force-displacement transducer precalibrated with standard weights on a Grass model 5D polygraph. The cylindrical segments are bathed in 25 mL of PSS in a water jacketed tissue bath at 37 °C. The bath solution is bubbled continuously with a mixture of 95% O2-5% CO2. An initial resting tension of 10 g is set during a 2-hour equilibration period. After the equilibration, three to four successive contraction-relaxation cycles are induced with 35 mM KCl and subsequent washes with PSS until reproducible contractions are obtained. After the final response reached and maintained steady tension (16-25 g above resting tension), a cumulative dose-response curve for Felodipine is obtained. Additional aliquots of Felodipine are added only after the response to the previous dose has plateaued. The concentration of Felodipine that half-maximally relaxes the coronary from KCl-induced contraction (IC50) is determined from dose response curv

Animal Study: [7]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Johnson JD, et al. J Pharmacol Exp Ther, 1983, 226(2), 330-334.

[2] R?dler S, et al. J Mol Cell Cardiol, 1995, 27(10), 2295-2302.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
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 Analytical  ...more 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
NCT01238705 Recruiting Hypertension|Sexual Dysfunction LanZhou University April 2008 Phase 4

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Chemical Information

Download Felodipine SDF
Molecular Weight (MW) 384.25
Formula

C18H19Cl2NO4

CAS No. 72509-76-3
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 77 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 72 mg/mL (187 mM)
* <1 mg/ml means slightly soluble or 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.

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Tech Support & FAQs

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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