Gliclazide
Gliclazide is a sulfonylurea compound that inhibits sulfonylurea 1 (SUR1) receptors, exhibiting anti-diabetic and antioxidative activities. Inhibition of these receptors closes K+ ion channels, inducing cell membrane depolarization, altering Ca2+ homeostasis, and stimulating insulin release. In vitro, gliclazide inhibits H2O2-induced mitochondrial damage and apoptosis, decreasing oxidative stress.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18927461
| Cas No. |
21187-98-4 |
|---|---|
| Purity |
≥98% |
| Formula |
C15H21N3O3S |
| Formula Wt. |
323.41 |
| Chemical Name |
N-[[(Hexahydrocyclopenta[c]pyrrol-2(1H)-yl)amino]- carbonyl]-4-methylbenzenesulfonamide |
| IUPAC Name |
1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea |
| Synonym |
Diamicron; Glimicron; Nordialex |
| Melting Point |
180-182°C |
| Solubility |
Insoluble in water. Soluble in dichloromethane. |
| Appearance |
White Crystal Powder |
Proks P, de Wet H, Ashcroft FM. Molecular mechanism of sulphonylurea block of K(ATP) channels carrying mutations that impair ATP inhibition and cause neonatal diabetes. Diabetes. 2013 Nov;62(11):3909-19. PMID: 23835339.
Sliwinska A, Rogalska A, Szwed M, et al. Gliclazide may have an antiapoptotic effect related to its antioxidant properties in human normal and cancer cells. Mol Biol Rep. 2012 May;39(5):5253-67. PMID: 22183301.
Lawrence CL, Proks P, Rodrigo GC, et al. Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells. Diabetologia. 2001 Aug;44(8):1019-25. PMID: 11484080.
