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Purity: ≥98%
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.
| ln Vitro |
There are no significant differences in viability between the control cells and the cells treated with 100 μM of FAC or 1 and 10 μM of nifedipine. Nifedipine (BAY-a-1040) (1, 10, or 100 μM) significantly increases the iron level in WKPT-0293 Cl.2 cells. Nifedipine (BAY-a-1040) (10 or 100 μM) significantly lowers the viability of the WKPT-0293 Cl.2 Cells. Treatment of nifedipine (10 or 100 μM) plus FAC induces a significant reduction in cell viability. In WKPT-0293 Cl.2 cells, nifedipine treatment also upregulates the expression of TfR1, DMT1+IRE, and DMT1-IRE. Furthermore, co-administration of 100 μM nifedipine and 100 μM FAC results in upregulation of TfR1, DMT1+IRE, and DMT1-IRE expression in WKPT-0293 Cl.2 cells[2]. In the midrange of concentrations, nifedipine plus ritodrine significantly inhibits contractility more than either medication alone. A considerably higher inhibition is produced by nifedipine plus atosiban or nitroglycerin combined than by either drug alone, but not by nifedipine plus atosiban. The inhibitory effect of each drug is lessened when nifedipine and NS-1619 (Ca2+-activated K+ [BKCa] channel opener) are taken together[3]. At 2 μM, nifedipine (BAY-a-1040) dramatically suppresses the growth and sporulation of P. capsici mycelial cells. Calcium is required for the inhibition of mycelial growth caused by nifedipine (BAY-a-1040). P. capsici's sensitivity to H2O2 is increased by nifedipine (0.5 μM) in a calcium-dependent way[4].
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| ln Vivo |
At the conclusion of the fourth week, the BL dimensions (BLi and BLk), MD dimensions (MDk), and vertical dimensions (VHi and VHk) of rats treated with Nifedipine (BAY-a-1040) (50 mg/kg) and CsA show a significant (P < 0.05) increase[1].
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| References |
[1]. Ratre MS, et al. Effect of azithromycin on gingival overgrowth induced by cyclosporine A + nifedipine combination therapy: A morphometric analysis in rats. J Indian Soc Periodontol. 2016 Jul-Aug;20(4):396-401.
[2]. Carvajal JA, et al. The Synergic In Vitro Tocolytic Effect of Nifedipine Plus Ritodrine on Human Myometrial Contractility. Reprod Sci. 2017 Apr;24(4):635-640. [3]. Yu SS, et al. Nifedipine Increases Iron Content in WKPT-0293 Cl.2 Cells via Up-Regulating Iron Influx Proteins. Front Pharmacol. 2017 Feb 13;8:60 [4]. Liu P, et al. The L-type Ca(2+) Channel Blocker Nifedipine Inhibits Mycelial Growth, Sporulation, and Virulence of Phytophthora capsici. Front Microbiol. 2016 Aug 4;7:1236 |
| Molecular Formula |
C17H18N2O6
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| Molecular Weight |
346.33
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| CAS # |
21829-25-4
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| Related CAS # |
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| SMILES |
O(C([H])([H])[H])C(C1=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C(C(=O)OC([H])([H])[H])C1([H])C1=C([H])C([H])=C([H])C([H])=C1[N+](=O)[O-])=O
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| InChi Key |
HYIMSNHJOBLJNT-UHFFFAOYSA-N
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| 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
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| Chemical Name |
dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8874 mL | 14.4371 mL | 28.8742 mL | |
| 5 mM | 0.5775 mL | 2.8874 mL | 5.7748 mL | |
| 10 mM | 0.2887 mL | 1.4437 mL | 2.8874 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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