| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H28N4O4S |
| Molecular Weight | 456.558 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C1=NOC(=N1)N2CCC(COC3=CC=C(N=C3)C4=CC=C(C=C4)S(C)(=O)=O)CC2
InChI
InChIKey=AYJRTVVIBJSSKN-UHFFFAOYSA-N
InChI=1S/C23H28N4O4S/c1-16(2)22-25-23(31-26-22)27-12-10-17(11-13-27)15-30-19-6-9-21(24-14-19)18-4-7-20(8-5-18)32(3,28)29/h4-9,14,16-17H,10-13,15H2,1-3H3
GSK1292263 (GSK263) (5-[({1-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl}methyl)oxy]-2-[4-(methylsulfonyl)phenyl]pyridine) is a potent and selective agonist at the rodent and human GPR119 receptors that was discovered at GlaxoSmithKline. It has a pEC50 = 6.8 for human, rat and mouse GPR119 receptors expressed in an in vitro reporter assay, and a pEC50 = 8.5 for the stimulation of GLP-1 secretion from GLUTag cells. Like other GPR119 agonists, GSK1292263 increases glucose-sensitive insulin secretion, improves glucose tolerance and enhances the secretion of gut hormones in normal rats. GSK1292263 has finished Phase II clinical trial for Diabetes Mellitus, Type 2.
Originator
Approval Year
Sourcing
PubMed
Patents
ACTIVE MOIETY
