Chemical Probes logo
Repaglinide | Repaglinide : 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
  • IC50:106 nM
  • IC50:800 nM
KCNJ11
  • IC50:106 nM
  • IC50:800 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - SLC22A1: 9,200 nM

Potency Assay Off-Target:
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK29 ...
Selectivity Assessment Description:
Inactive against CYP3A4, CYP2C8 and CYP3A5; data from ChEMBL and Probe Miner (http://probeminer.icr. ...

Potency
Cellular
In Vitro

ABCC8

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.2337/diabetes.51.9.2789

KCNJ11

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.2337/diabetes.51.9.2789

In Vivo Validations

Rat
Dose: 1 mg/kg
Route of delivery: Oral
Organ of interest (O): Pancreas
Target engagement assay: Indirect; repaglinide decreased blood glucose with an ED50=15.6 ug/kg.

DOI Reference: 10.1016/j.bmcl.2004.07.059

Orthogonal Probes def

Glyburide

Chemical Information

Molecular Formula C27H36N2O4
SMILEs CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O
InChI InChI=1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
Molecular weight 452.27 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 69

Vendors

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

Expert Reviews

by SERP
(on 29 Apr 2020 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 15 May 2020 )
Cellular Use Rating
In Model Organisms
Repaglinide is a member of the meglitinide family of insulin secretagogues. Like the sulfonylurea class of anti-diabetes drugs, Repaglinide binds and inhibits the KATP (ATP-dependent potassium channel)...
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