Chemical Probes logo
Glyburide | Glyburide : Inhibitor of ABCC8, KCNJ11
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
ABCC8
  • IC50:4.3 nM
  • EC50:3 nM
KCNJ11
  • IC50:4.3 nM
  • EC50:3 nM
Inhibitor
--

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - ABCC9: 220 nM, SLCO1B1: 1,400 nM, ABCB11: 5,300 nM

Potency Assay Off-Target:
These are all values taken from ChEMBL. Please check ChEMBL and/or Probe Miner (http://probeminer.ic ...
Selectivity Assessment Description:
Glyburide has been evaluated against CYPs (PMID: 12920163) with IC50s >40 uM, except CYP2C9 (IC50=2. ...
In Vitro Selectivity Assessment
Selectivity Assessment Description:
The compound is inactive against hERG, CFTR (PMID: 8770056) and a few other targets. Please check Ch ...

Potency
Cellular
In Vitro

ABCC8

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.metabol.2012.07.010

KCNJ11

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.metabol.2012.07.010

In Vivo Validations

Rat, Mouse
Dose: 0.4, 1, 10 mg/Kg
Route of delivery: Oral
Organ of interest (O): Heart, pancreas

DOI Reference: 10.1016/0024-3205(93)90448-C

Orthogonal Probes def

Repaglinide

Chemical Information

Molecular Formula C23H28ClN3O5S
SMILEs COc1ccc(Cl)cc1C(=O)NCCc1ccc(S(=O)(=O)NC(=O)NC2CCCCC2)cc1
InChI InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
Molecular weight 493.14 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 61

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 15 May 2020 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 2 Jun 2020 )
Cellular Use Rating
In Model Organisms
Serum Glibenclamide in Diabetic Patients, and Influence of Food on the Kinetics and Effects of Glibenclamide is not useful to include for consideration as chemical probe (although is useful to list...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria