research use only
Cat.No.S1971
| Related Targets | CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR |
|---|---|
| Other Potassium Channel Inhibitors | TRAM-34 Nigericin Sophocarpine ML133 HCl Hydralazine HCl Gliquidone PAP-1 E-4031 dihydrochloride Ajmaline NS8593 Hydrochloride |
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In vitro |
DMSO
: 42 mg/mL
(198.89 mM)
Ethanol : 34 mg/mL Water : 21 mg/mL |
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In vivo |
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| Molecular Weight | 211.17 | Formula | C8H9N3O4 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 65141-46-0 | Download SDF | Storage of Stock Solutions |
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| Synonyms | SG-75 | Smiles | C1=CC(=CN=C1)C(=O)NCCO[N+](=O)[O-] | ||
| Targets/IC50/Ki |
Potassium channel
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| 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. This compound 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. This chemical suppresses TUNEL positivity, cytochrome c translocation, caspase-3 activation and dissipation of mitochondrialinner membrane potential (Delta(Psi)(m)). It 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). This compound activates a weakly inwardly-rectifying, glibenclamide-sensitive 80 pS K+ channel in both the transfected cells. It preferentially activates the K(ATP) channels containing SUR2B in HEK293T cells. This chemical significantly suppresses the number of cells with TUNEL-positive nuclei and the increase in caspase-3 activity induced by 20 mM H2O2. It prevents the loss of DeltaPsim induced by H2O2 in a concentration-dependent manner.
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| 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.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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