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Nisoldipine Calcium Channel inhibitor

Cat.No.S1748

Nisoldipine (Sular, BAY K 5552) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
Nisoldipine Calcium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 388.41

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Quality Control

Batch: Purity: 99.69%
99.69

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (198.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble

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

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Chemical Information, Storage & Stability

Molecular Weight 388.41 Formula

C20H24N2O6

 Storage (From the date of receipt)
CAS No. 63675-72-9 Download SDF Storage of Stock Solutions

Synonyms BAY K 5552 Smiles CC1=C(C(C(=C(N1)C)C(=O)OCC(C)C)C2=CC=CC=C2[N+](=O)[O-])C(=O)OC

Mechanism of Action

Features
A member of the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs.
Targets/IC50/Ki
L-type Cav1.2
10 nM
In vitro
Nisoldipine is a potent blocker of L-type calcium channels. This compound binds directly to inactive calcium channels stabilizing their inactive conformation Similar to other DHP CCBs. It displays selectivity for arterial smooth muscle cells due to great number of inactive channels and the α1 subunit of the channel. This chemical is about 30 times less selective for delayed-rectifier K+ channels than for L-type Ca2+ channels, which inhibits IKr (rapidly activating delayed-rectifier K+ current) with IC50 of 23 μM, and IKs (slowly activating delayed-rectifier K+ current)with IC50 of 40 μM in guinea-pig ventricular myocytes. It also displays antioxidant potency with IC50 of 28.2 μM both before and after the addition of active oxygen. This is tested by means of rat myocardial membrane lipid peroxidation with a nonenzymatic active oxygen-generating system (DHF/FeC13-ADP).
Kinase Assay
Binding experiments of electrophysiology
CHO cells expressing the subunit of the voltage-dependent L-type Ca2+ channel are cultrured in medium without serum in the presence of different concentrations of Nisoldipine. Then Ca2+ channel current elicited from a holding potential of -100 mV or -50 mV is recorded at room temperature with the whole-cell configuration of the patch-clamp method using the List EPC-7 patch-clamp amplifer and pClamp software. The concentration of this compound inhibiting 50% of the specific binding represents IC50.
In vivo
Nisoldipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. This results in vasodilation and an overall decrease in blood pressure, based on which this compound is used to treat mild to moderate essential hypertension, chronic stable angina and Prinzmetal's variant angina. It shows some ability in patients with Timothy syndrome having Cav1.2 missense mutation G406R with IC50 of 267 nM, which is helpful to treat TS.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8690410/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15454078/

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