Nisoldipine

Catalog No.S1748 Batch:S174801

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Technical Data

Formula

C20H24N2O6
Molecular Weight 388.41 CAS No. 63675-72-9
Solubility (25°C)* In vitro DMSO 78 mg/mL (200.81 mM)
Ethanol 78 mg/mL (200.81 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
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]
Features A member of the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs.

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[2]
  • 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.
Animal Study:[4]
  • Animal Models

    Male Wistar rats with chronic intragastric ethanol exposure

  • Dosages

    10 mg/kg

  • Administration

    Oral every day

Selleck's Nisoldipine has been cited by 6 publications

Calenduloside E protects against myocardial ischemia-reperfusion injury induced calcium overload by enhancing autophagy and inhibiting L-type Ca2+ channels through BAG3 [ Biomed Pharmacother, 2022, 145:112432] PubMed: 34798472
Deciphering COVID-19 host transcriptomic complexity and variations for therapeutic discovery against new variants [ iScience, 2022, 25(10):105068] PubMed: 36093376
Trypsin-Mediated Sensitization to Ferroptosis Increases the Severity of Pancreatitis in Mice [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X] PubMed: 34562639
Calcium channel blocker amlodipine besylate therapy is associated with reduced case fatality rate of COVID-19 patients with hypertension [ Cell Discov, 2020, 6(1):96] PubMed: 33349633
Calenduloside E suppresses calcium overload by promoting the interaction between L-type calcium channels and Bcl2-associated athanogene 3 to alleviate [ Journal of Advanced Research, 2020, 10.1016/j.jare.2020.10.005] PubMed: None
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 [ bioRxiv, 2020, 2020/9/20.4.7.30734] PubMed: 32511305

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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