Nisoldipine

Catalog No.S1748 Synonyms: BAY K 5552

Nisoldipine  Chemical Structure

Molecular Weight(MW): 388.41

Nisoldipine (Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

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Biological Activity

Description Nisoldipine (Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
Features A member of the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs.
Targets
L-type Cav1.2 [1]
10 nM
In vitro

Nisoldipine is a potent blocker of L-type calcium channels. Nisoldipine binds directly to inactive calcium channels stabilizing their inactive conformation Similar to other DHP CCBs. Nisoldipine displays selectivity for arterial smooth muscle cells due to great number of inactive channels and the α1 subunit of the channel. [1] Nisoldipine 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. [2] Nisoldipine 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). [3]

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 Nisoldipine is used to treat mild to moderate essential hypertension, chronic stable angina and Prinzmetal's variant angina. [4] Nisoldipine 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. [5]

Protocol

Kinase Assay:[1]
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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 competitor inhibiting 50% of the specific binding represents IC50.
Cell Research:[2]
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  • Cell lines: Ventricular myocytes
  • Concentrations: Dissolved in DMSO, final concentration 10-100 μM
  • Incubation Time: 8-10 minutes
  • Method: The myocytes are bathed in normal Tyrode's solution, held at -80 mV, and depolarised after 200-ms prepulses (-40mV) to more positive potentials for 500 ms at 0.1 Hz, tail currents are recorded on repolarisations to -40mV. The myocytes are exposed to 10-100 mM Nisoldipine for 8-10 minutes. Then the whole-cell membrane currents are recorded using an EPC-7 amplifier.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Male Wistar rats with chronic intragastric ethanol exposure
  • Formulation: Dissolved in DMSO and diluted in saline
  • Dosages: 10 mg/kg
  • Administration: Oral every day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (198.24 mM)
Ethanol 60 mg/mL warmed (154.47 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 388.41
Formula

C20H24N2O6

CAS No. 63675-72-9
Storage powder
in solvent
Synonyms BAY K 5552

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00985660 Completed Healthy Mylan Pharmaceuticals June 2007 Phase 1
NCT00979537 Completed Healthy Mylan Pharmaceuticals March 2007 Phase 1
NCT00730197 Completed Healthy Mylan Pharmaceuticals February 2007 Phase 1
NCT00311870 Completed Diabetic Nephropathy Steno Diabetes Center|Bayer March 1993 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID