product name Nicorandil
Description: Nicorandil (also known as RP-46417, SG-75, and Adancor) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). .Nicorandil is a vasodilatory drug used to treat angina. Nicorandil causes vasodilatation of arterioles and large coronary arteries. Nicorandals nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.
References: J Am Coll Cardiol. 2000 Feb;35(2):514-8; Mol Cell Biochem. 2003 Jan;243(1-2):133-8.
211.17
Formula
C8H9N3O4
CAS No.
65141-46-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 42 mg/mL (198.9 mM)
Water: 17 mg/mL (80.5 mM)
Ethanol: 42 mg/mL (198.9 mM)
Solubility (In vivo)
Synonyms
SG-75
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Am Coll Cardiol. 2000 Feb;35(2):514-8; Mol Cell Biochem. 2003 Jan;243(1-2):133-8. |
