N7634
Nifedipine
≥98% (HPLC), powder, L-type Ca²⁺ channel blocker
Synonyme(s) :
1,4-Dihydro-2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester
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About This Item
Nom du produit
Nifedipine, ≥98% (HPLC), powder
form
powder
color
yellow
InChI key
HYIMSNHJOBLJNT-UHFFFAOYSA-N
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 string
COC(=O)C1=C(C)NC(C)=C(C1c2ccccc2[N+]([O-])=O)C(=O)OC
assay
≥98% (HPLC)
solubility
DMSO: soluble
ethanol: soluble
originator
Bayer
storage temp.
2-8°C
Quality Level
Gene Information
human ... ADORA2A(135), ADORA3(140), CACNA1C(775), CACNA1D(776), CACNA1F(778), CACNA1S(779), CACNA2D1(781), CYP1A2(1544), KCNH1(3756), TTR(7276)
mouse ... Cacna1c(12288)
rat ... Adora1(29290), Adora2a(25369), Cacna1c(24239), Cacna1d(29716), Kcnj1(24521), Kcnn4(65206), Tbxas1(24886)
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Catégories apparentées
Application
- to evaluate its effect on myenteric neuronal calcium current through R-type calcium channel in guinea pig small intestine
- to evaluate the neuroprotective effect of L-type calcium channel blockers in cholinergic and dopaminergic neurons
- to identify the effect of co-administration of nifedipine (anti-hypertensive drug) along with hypoglycemic drug on human umbilical vein cells (HUVECs)
Biochem/physiol Actions
Features and Benefits
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Classe de stockage
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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If available for a given product, the recommended re-test date or the expiration date can be found on the Certificate of Analysis.
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What is the solubility of Product N7634, Nifidipine?
Nifedipine can be dissolved in DMSO at 50 mg/ml1. It is sparingly soluble in absolute ethanol2. Herembert, T. et al., dissolved nifedipine in absolute ethanol (no concentration reported); the maximum ethanol concentration in cultures was 0.2% without any effect of solvent on the cells3. Nifedipine is soluble (g/L, at 20°C) in the following solvents: acetone, 250; methylene chloride, 160; chloroform, 140; ethyl acetate, 50; methanol, 26; ethanol, 17.4 It is practically insoluble in water. The solubilities at 37°C in buffer solutions of different pH values are: pH 4, 0.0058 g/L; pH 7, 0.0056 g/L; pH 9.0, 0.0078 g/L; pH 13, 0.006 g/L1. References: 1. Ali, S.L., Analytical Profiles of Drug Substances, 18, 221, (1989). 2. Martindale, The Extra Pharmacopoeia, 30th ed., 374, (1993). and 3. Herembert, T. et al. Brit. J. Pharmacol., 114, 1703, (1995).
Are there any recommended dosages for Product N7634, Nifidipine, in vivo and in vitro?
Nifedipine is reported to inhibit Ca2+-sensitive K+ channels at 100 μM1. Doses for different animals have been reported2,3. In randomly growing cultures of aortic cells of rats, nifedipine at 10 μM inhibited cell proliferation. References: 1. Thomas-Young, R.J. et al. Biochim. Biophys. Acta, 1146, 81, (1993). 2. Drug Dosages In Laboratory Animals: A Handbook, 3rd ed., Telford Press. and 3. Borchard, R.E. et al. Drug Dosage in Laboratory Animals, A Handbook, Third Edition, p. 315, The Telford Press, (1990).
What is the half life of Product N7634, Nifidipine, in vivo?
After administration by the mouth, the half-life is 2 to 5 hours 1. In plasma, about 92-98% binds to plasma proteins. Nifedipine is completely metabolized. About 70% of a dose is excreted in the urine in 24 hours as metabolites including 5-methoxycarbonyl-2,6-dimethyl-4-(2-nitrophenyl) pyridine-3-carboxylic acid; dimethyl 2,6-dimethyl-4-(2-nitrophenyl pyridine-3,5-dicarboxylate and 2-hydroxymethyl-5-methoxycarbonyl-6-methyl-4-(2-nitrophenyl) pyridine-3-carboxylic acid and its lactone derivative. Up to 15% of a dose is eliminated in the feces as metabolites in 4 days 2. References: 1. Martindale, 29th ed., pgs. 1509-1513. 2. Clarke's Isolation and Identification of Drugs., 2nd ed., p. 811.
Are there any recommended conditions that Product N7634, Nifidipine, should be used in?
When exposed to daylight and certain wavelengths of artificial light, nifedipine readily converts to a nitrosophenylpyridine derivative. Exposure to ultra-violet light leads to the formation of a nitrophenylpyridine derivative. Therefore, USP recommends that assays be performed in the dark or under golden fluorescent or other low actinic light. Low actinic glassware should be used1.
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