Licensed by Pfizer Catalog No.S1808
Molecular Weight(MW): 346.33
Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.
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|Description||Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.|
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. 
|In vivo||Nifedipine (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. |
-  Ding Y, et al. J Pharmacol Exp Ther,?000, 292(2), 606-609.
-  Zhang X, et al. J Pharmacol Exp Ther,?997, 281(3), 1247-1256.
-  Hirata A, et al. Br J Pharmacol,?000, 131(8), 1521-1530.
|In vitro||DMSO||69 mg/mL (199.23 mM)|
|Ethanol||15 mg/mL (43.31 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02047019||Withdrawn||Hypertension||Bayer||December 2017||Phase 3|
|NCT03005496||Not yet recruiting||PreTerm Birth||Indonesia University||December 2016||Phase 4|
|NCT02940548||Recruiting||Hypertension||Jing Liu|Bayer|Peking University Peoples Hospital||December 2016||Phase 4|
|NCT02912910||Withdrawn||Hypertension||St. Louis University||September 2016||--|
|NCT02902354||Withdrawn||Tocolysis With Nifedipine||St. Louis University||September 2016||--|
|NCT02933593||Withdrawn||Hypertension||St. Louis University||August 2016||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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