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rac-trans-4-hydroxy Glyburide (Synonyms: 4-trans-hydroxycyclohexyl Glyburide, 4-trans-hydroxy Glibenclamide)

Katalog-Nr.GC48461

An active metabolite of glyburide

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rac-trans-4-hydroxy Glyburide Chemische Struktur

Cas No.: 23155-00-2

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500µg
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1mg
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5mg
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents

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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