Nifedipine Calcium Channel inhibitor

Cat.No.S1808

Nifedipine is a dihydropyridine calcium channel blocker, used to lower hypertension and to treat angina.
Nifedipine Calcium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 346.33

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 346.33 Formula

C17H18N2O6

Storage (From the date of receipt) 2 years 4°C(in the dark) powder
CAS No. 21829-25-4 Download SDF Storage of Stock Solutions

Synonyms BAY-a-1040 Smiles CC1=C(C(C(=C(N1)C)C(=O)OC)C2=CC=CC=C2[N+](=O)[O-])C(=O)OC

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (199.23 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
calcium channel [1]
In vitro
Nifedipine causes a significant concentration-dependent increase in eNOS protein expression by cultured human coronary artery endothelial cells. [1] This compound antagonizes L-type Ca+ channels found throughout the cardiovascular system, but also blocks Kv channels, which are members of the same supergene family. [2] It 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). This chemical suppresses the levels of proliferative cell nuclear antigen (PCNA) dose-dependently in both VSMC and balloon-injured thoracic aortae in VSMC. [3]
In vivo
Nifedipine (3 mg/kg) slightly lowers the level of systolic and/or diastolic blood pressure or increased the heart rate in rats. [3] This compound (1 μm) produces a maximal inhibition of the store-operated pathway in choroidal arteriolar smooth muscle. [4] This chemical (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. It (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. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/11313433/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9920200/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05096728 Completed
Preeclampsia With Severe Features
Ohio State University
December 1 2021 --
NCT04392375 Completed
Preeclampsia Severe
Ohio State University
June 9 2020 Phase 4
NCT03695107 Unknown status
Chronic Kidney Diseases
The Third Xiangya Hospital of Central South University
October 2 2019 --
NCT02902354 Withdrawn
Tocolysis With Nifedipine
St. Louis University
September 2016 Not Applicable
NCT03710395 Unknown status
Drug Transporter
Natalia Valadares de Moraes|Hospital das Clínicas de Ribeirão Preto|Universidade Estadual Paulista Júlio de Mesquita Filho
December 14 2015 Phase 4

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