Name: Felodipine
Brand: Selleck Chemicals
SKU: S1885
Availability: InStock
Rating: 5 (4 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	CFTR CRM1 CD markers AChR Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Calcium Channel Inhibitors	Bay K 8644 Tetrandrine Nilvadipine Flunarizine 2HCl Cilnidipine YM-58483 (BTP2) Ionomycin Imperatorin Manidipine 2HCl Astragaloside A

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
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
H9C2 cells	Function assay		Inhibition of L-VDCC in rat H9C2 cells assessed as effect on calcium level by Fluo-4 fluorescence assay
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (200.39 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 72 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.850mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 77 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.900mg/ml (4.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 38 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	384.25	Formula	C₁₈H₁₉Cl₂NO₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	72509-76-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGH-869			Smiles	CCOC(=O)C1=C(NC(=C(C1C2=C(C(=CC=C2)Cl)Cl)C(=O)OC)C)C

Mechanism of Action

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/IC₅₀/Ki	L-type calcium channel 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). This compound 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. It blocks the muscarinic receptor-mediated (carbachol) Ca²⁺-dependent contraction of guinea pig ileum longitudinal smooth muscle (GPILSM) with an IC50 of 1.45 nM. This chemical 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. It (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. It modestly blocks the Ca_v3.2 T-type Ca²⁺-channel with an IC50 of 6.8 μM.
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. Administration of this compound 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/6875846/ [2] https://pubmed.ncbi.nlm.nih.gov/8576944/ [3] https://pubmed.ncbi.nlm.nih.gov/8917646/ [4] https://pubmed.ncbi.nlm.nih.gov/9774369/ [5] https://pubmed.ncbi.nlm.nih.gov/11744032/ [6] https://pubmed.ncbi.nlm.nih.gov/18974361/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Felodipine Calcium Channel inhibitor

Chemical Structure

Molecular Weight: 384.25