rac-trans-4-hydroxy Glyburide (Synonyms: 4-trans-hydroxycyclohexyl Glyburide, 4-trans-hydroxy Glibenclamide) |
| カタログ番号GC48461 |
グリブライドの活性代謝物質
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 23155-00-2
Sample solution is provided at 25 µL, 10mM.
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rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2 It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1 rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.2
1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes responsible for the biotransformation of glyburideBiochem. Pharmacol.78(12)1483-1490(2009) 2.Hill, R.A., Rudra, S., Peng, B., et al.Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomesBioorg. Med. Chem.11(9)2099-2113(2003)
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