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    Felodipine (CGH869)
    Felodipine (CGH869)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0619
    CAS #: 72509-76-3 Purity ≥98%

    Description: Felodipine (formerly also known as CGH-869; trade names Plendil, Renedil etc.), a marketed anti-hypertensive drug, is a potent, selective and long-acting L-type Ca2+ channel blocker (CCB) of the 1,4-dihydropyridine (DHP) class with an IC50 of 0.15 nM. It was approved to treat high blood pressure in 1988. Felodipine is described to inhibit cytokine-induced NO and superoxide production as well as cytokine-induced NO synthase (NOS) mRNA induction, and is suggested to act as a scavenger of superoxide and not an inhibitor of inducible NOS induction. This indicates that Felodipine further protects the vasculature against endogenous free radical generation during inflammatory responses.

    References: J Pharmacol Exp Ther. 1983 Aug;226(2):330-4; J Mol Cell Cardiol. 1995 Oct;27(10):2295-302.

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    Molecular Weight (MW)384.25 
    FormulaC18H19Cl2NO4 
    CAS No.72509-76-3 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 77 mg/mL (200.4 mM) 
    Water: <1 mg/mL
    Ethanol: 77 mg/mL (200.4 mM) 
    Other info

    Chemical Name: (RS)-3-ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

    InChi Key: RZTAMFZIAATZDJ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C18H19Cl2NO4/c1-5-25-18(23)14-10(3)21-9(2)13(17(22)24-4)15(14)11-7-6-8-12(19)16(11)20/h6-8,15,21H,5H2,1-4H3

    SMILES Code: O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC(Cl)=C2Cl)OCC

    SynonymsCGH-869; Perfudal, Plendil, Renedil, Felodipine,CGH 869; Felobeta, CGH869; Agon, Felo-Puren,Felocor, Felodipin,  Felodur Felogamma, Fensel, Flodil, Modip, Munobal, 


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    In Vitro

    In vitro activity: 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). 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. 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. 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. 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. Felodipine modestly blocks the Cav3.2 T-type Ca2+-channel with an IC50 of 6.8 μM.


    Cell Assay: 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 gene

    In VivoOral 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 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. 
    Animal modelRats
    Formulation & DosageOral
    References

    J Pharmacol Exp Ther. 1983 Aug;226(2):330-4; J Mol Cell Cardiol. 1995 Oct;27(10):2295-302. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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