Felodipine

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.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 310 In stock
USD 670 In stock

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective Calcium Channel Inhibitors

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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.
Targets
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]

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
+ Expand
  • 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 <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 384.25
Formula

C18H19Cl2NO4

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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02744872 Recruiting 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Calcium Channel Signaling Pathway Map

Related Calcium Channel Products

Tags: buy Felodipine | Felodipine supplier | purchase Felodipine | Felodipine cost | Felodipine manufacturer | order Felodipine | Felodipine distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID