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    Nifedipine (BAY-a-1040)
    Nifedipine (BAY-a-1040)

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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 #: V1289
    CAS #: 21829-25-4Purity ≥98%

    Description: Nifedipine (Adalat, Procardia, Bay-1040, BAY-a-1040; Cordipin, Corinfar, Bay 1040) is a dihydropyridine calcium channel blocker (CCB) with antihypertensive effects. It has been used to lower blood pressure and to treat angina, Raynaud's phenomenon, and premature labor. Nifedipine targets L-type voltage-sensitive calcium channels. Nifedipine is a vasodilator that is selective for inotropic over chronotropic cardiac effects. Nifedipine causes a significant concentration-dependent increase in eNOS protein expression by cultured human coronary artery endothelial cells. Nifedipine antagonizes L-type Ca+ channels found throughout the cardiovascular system, but also blocks Kv channels, which are members of the same supergene family.

    References: J Pharmacol Exp Ther. 2000 Feb;292(2):606-9; Br J Pharmacol. 2000 Dec;131(8):1521-30.

    Related CAS#: 1188266-14-9 (Nifedipine D6); 21881-77-6 (m-Nifedipine, impurity of Nifedipine)

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    Molecular Weight (MW)346.33 
    FormulaC17H18N2O6 
    CAS No.21829-25-4  (Nifedipine);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 69 mg/mL (199.2 mM)
    Water: <1 mg/mL
    Ethanol: 15 mg/mL (43.3 mM)
    Other infoIUPAC/Chemical Name: dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
    InChi Key: HYIMSNHJOBLJNT-UHFFFAOYSA-N
    InChi Code: InChI=1S/C17H18N2O6/c1-9-13(16(20)24-3)15(14(10(2)18-9)17(21)25-4)11-7-5-6-8-12(11)19(22)23/h5-8,15,18H,1-4H3
    SMILES Code: O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC=C2[N+]([O-])=O)OC
    SynonymsBAY-a 1040; BAY a-1040; Adalat, Procardia, Bay-1040, BAY-a-1040; Cordipin, Corinfar, Bay 1040, Bay1040


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    In Vitro

    In vitro activity: Nifedipine causes a significant concentration-dependent increase in eNOS protein expression by cultured human coronary artery endothelial cells. Nifedipine antagonizes L-type Ca+ channels found throughout the cardiovascular system, but also blocks Kv channels, which are members of the same supergene family. Nifedipine dose-dependently decreases the values of [(3)H]-thymidine incorporation and total cellular protein content as well as the levels of phosphorylated extracellular signal-regulated protein kinase (ERK) 1/2, mitogen-activated protein kinase kinase (MEK) 1/2, and even the phosphorylation of Pyk2, in vascular smooth muscle cells (VSMC). Nifedipine suppresses the levels of proliferative cell nuclear antigen (PCNA) dose-dependently in both VSMC and balloon-injured thoracic aortae in VSMC.


    Cell Assay: Cell viability is assessed using an MTT assay. Briefly, a total of 25 μL MTT (1 g/L in PBS) is added to each well before incubation is conducted at 37°C for 4 h. The assay is stopped by the addition of a 100 μL lysis buffer (20% SDS in 50% N’Ndimethylformamide, pH 4.7). Optical density (OD) is measured at the 570 nm wavelength by the use of an ELX-800 microplate assay reader and the results are expressed as a percentage of the absorbance measured in the control cells.

    In VivoNifedipine (3 mg/kg) slightly lowers the level of systolic and/or diastolic blood pressure or increased the heart rate in rats. Nifedipine (1 μm) produces a maximal inhibition of the store-operated pathway in choroidal arteriolar smooth muscle. Nifedipine (20 and 40 mg/kg) markedly prevents the HCl plus ethanol-induced gastric mucosal injury and the increase in the content of thiobarbituric acid-reactive substances in the injured mucosa in rats. Nifedipine (20 and 40 mg/kg) dose-dependently promotes the ulcer healing and inhibites the increase in the content of thiobarbituric acid-reactive substances in the ulcerated mucosa in rats. 
    Animal model Rats
    Formulation & Dosage All the 30 rats are randomLy distributed into three equal groups of ten animals each. Group 1 (control) receive olive oil for the 8 weeks. Group 2 and Group 3 receive a combination of CsA (30 mg/kg body weight) and Nf (50 mg/kg body weight) in olive oil for 8 weeks. In Group 3 rats, Azi (10 mg/kg body weight) is added to this regimen, in the 5th week. The total study period is 8 weeks.
    ReferencesJ Pharmacol Exp Ther. 2000 Feb;292(2):606-9; Br J Pharmacol. 2000 Dec;131(8):1521-30. 


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

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