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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
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Probe Summary

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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

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Expert Reviews

by SERP
(on 29 Apr 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public 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)...
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