Catalog No.S1971 Synonyms: SG-75
Molecular Weight(MW): 211.17
Nicorandil is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).
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(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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Choose Selective Potassium Channel Inhibitors
|Description||Nicorandil is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).|
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.  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).  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.  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. 
|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. |
-  Sato T, et al. J Am Coll Cardiol, 2000, 35(2), 514-518.
-  Akao M, et al. J Am Coll Cardiol, 2002, 40(4), 803-810.
-  Szczepanik AM, et al. J Pharmacol Exp Ther, 1996, 278(2), 913-920.
|In vitro||DMSO||42 mg/mL (198.89 mM)|
|Ethanol||42 mg/mL (198.89 mM)|
|Water||17 mg/mL (80.5 mM)|
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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|Merck Serono Co. Ltd. China||November 30 2016||Phase 4|
|NCT03445728||Enrolling by invitation||Myocardial Infarction|Percutaneous Coronary Intervention|Nicorandil||Chinese PLA General Hospital||February 24 2018||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||Unknown status||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|
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