Nicorandil

Catalog No.S1971 Synonyms: SG-75

Nicorandil Chemical Structure

Molecular Weight(MW): 211.17

Nicorandil is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 60 In stock
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2 Customer Reviews

  • (G) The fold change of C-peptide content after octreotide, nicorandil and nifedipine treatment. Octreotide, nicorandil and nifedipine decreased insulin secretion in wild-type, heterozygous mutated and homozygous mutated cells.

    Sci Rep, 2017, 7(1):3156. Nicorandil purchased from Selleck.

    Concentration-dependent effects of nicorandil to protect against stress and recovery (S/R)-induced cell injury and reactive oxygen species (ROS) production in nonaffected induced pluripotent stem cell (iPSC)-derived cardiomyocytes. The N-iCMs were subjected to 2 hours of oxidative stress followed by recovery. Protective effects of different concentrations of nicorandil (0.1, 1, 10, and 100 μmol/L) on cell injury and ROS production were assessed after 4 hours of recovery by measuring lactate dehydrogenase (LDH) release into the supernatant and evaluating dihydroethidium (DHE) fluorescent intensity, respectively. A, Stress induces an increase in LDH release in N-iCMs, which is mitigated by 10 and 100 μmol/L nicorandil but not 0.1 and 1 μmol/L. B, Stress induced an increase in ROS levels as indicated by DHE fluorescence, which is abolished by 10 and 100 μmol/L nicorandil but not 0.1 and 1 μmol/L. Data are mean ± standard error of the mean (SEM) of values from 3 independent experiments (n = 3/group). *P ≤ .05 versus control.

    J Cardiovasc Pharmacol Ther, 2016, 21(6):549-562. . Nicorandil purchased from Selleck.

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Biological Activity

Description Nicorandil is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).
Targets
Potassium channel [1]
In vitro

Nicorandil (100 mM) increases Flavoprotein oxidation but not membrane current; a 10-fold higher concentration recruits both mitoK(ATP) and surfaceK(ATP) channels. Nicorandil bluntes the rate of cell death in a pelleting model of ischemia; this cardioprotective effect is prevented by the mitoK(ATP) channel blocker 5-hydroxydecanoate but is unaffected by the surfaceK(ATP) channel blocker HMR1098. [1] Nicorandil (100 mM) suppresses TUNEL positivity, cytochrome c translocation, caspase-3 activation and dissipation of mitochondrialinner membrane potential (Delta(Psi)(m)). Nicorandil prevents Delta(Psi)(m) depolarization in a concentration-dependent manner (EC(50) approximately 40 mM, with saturation by 100 mM), as shown by fluorescence-activated cell sorter analysis of cells stained with a fluorescent Delta(Psi)(m)-indicator, tetramethylrhodamine ethyl ester (TMRE). [2] Nicorandil activates a weakly inwardly-rectifying, glibenclamide-sensitive 80 pS K+ channel in both the transfected cells. Nicorandil preferentially activates the K(ATP) channels containing SUR2B in HEK293T cells. [3] Nicorandil (100 mM) significantly suppresses the number of cells with TUNEL-positive nuclei and the increase in caspase-3 activity induced by 20 mM H2O2. Nicorandil prevents the loss of DeltaPsim induced by H2O2 in a concentration-dependent manner. [4]

In vivo Nicorandil (2.5 mg/kg daily, p.o.) combined with Amlodipine (5.0 mg/kg daily, p.o.) for 3 days significantly prevents these alterations and restored the enzyme activities to near normal in rats. [5]

Protocol

Solubility (25°C)

In vitro DMSO 42 mg/mL (198.89 mM)
Ethanol 42 mg/mL (198.89 mM)
Water 17 mg/mL (80.5 mM)

* 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 211.17
Formula

C8H9N3O4

CAS No. 65141-46-0
Storage powder
Synonyms SG-75

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03010423 Recruiting Non-obstructive Coronary Artery Disease Merck KGaA November 2016 Phase 4
NCT02809456 Enrolling by invitation Radiation Pneumonitis Taipei Medical University WanFang Hospital July 2016 Phase 2
NCT02449070 Recruiting Myocardial Infarction Pusan National University Hospital|JW Pharmaceutical May 2015 Phase 3
NCT02435797 Recruiting Coronary Heart Disease Xuzhou Central Hospital April 2015 Phase 4
NCT02328521 Unknown status Angina, Unstable|Diabetes Mellitus Zhang Ying Qian|Chinese PLA General Hospital December 2014 Phase 4
NCT02254252 Completed Slow Coronary Flow|Normal, or Near Normal Coronary Angiography|Stable Angina Mashhad University of Medical Sciences March 2012 Phase 4

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Potassium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID