4-trans-Hydroxy-glibenclamide

Rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide (HY-15206) . It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. 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.

Product Specifications

CAS Number

[23155-00-2]

Product Name Alternative

4-trans-hydroxycyclohexyl Glyburide; 4-trans-hydroxy Glibenclamide

UNSPSC

12352005

Hazard Statement

H315-H319-H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/4-trans-hydroxy-glibenclamide.html

Smiles

O=C(NCCC1=CC=C(S(=O)(NC(N[C@H]2CC[C@H](O)CC2)=O)=O)C=C1)C3=CC(Cl)=CC=C3OC

Molecular Formula

C23H28ClN3O6S

Molecular Weight

510.00

Precautions

P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362+P364-P403+P233-P405-P501

References & Citations

[1]Zharikova, et al. Identification of the major human hepatic and placental enzymes responsible for the biotransformation of glyburide. Biochem. Pharmacol. 78 (12), 1483-1490 (2009) .