Nicorandil

Synonyms: SG-75

Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).

Nicorandil Chemical Structure

Nicorandil Chemical Structure

CAS No. 65141-46-0

Purity & Quality Control

Nicorandil Related Products

Biological Activity

Description Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).
Targets
Potassium channel [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06249581 Active not recruiting
Chronic Stable Angina
Auxilius Pharma sp.z.o.o.
November 27 2023 Early Phase 1
NCT02809456 Unknown status
Radiation Pneumonitis
Taipei Medical University WanFang Hospital
July 2016 Phase 2
NCT01396395 Completed
Stable Angina|Coronary Disease
Merck KGaA Darmstadt Germany|Merck Serono Co. Ltd. China
September 2011 Phase 4

Chemical Information & Solubility

Molecular Weight 211.17 Formula

C8H9N3O4

CAS No. 65141-46-0 SDF Download Nicorandil SDF
Smiles C1=CC(=CN=C1)C(=O)NCCO[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 42 mg/mL ( (198.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 42 mg/mL

Water : 17 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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