DC7422 |
GSK1292263
|
GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. |
DC73445 |
ZB-16
|
ZB-16 (ZB40-0016) is a potent, selective GPR119 agonist, increase intracellular cAMP with EC50 of 7.25 nM, stimulates incretin secretion. |
DC73444 |
JTP-109192
|
JTP-109192 (JTP109192) is a potent GPR119 agonist with EC50 of 3.6. 4.5 and 5.2 nM for human, rat and mouse GPR119 respectively (increased intracellular cAMP levels). |
DC73443 |
HBK001
|
HBK001 (HBK-001) is a dual-target DPP4 inhibitor and GPR119 agonist with IC50 of 66 nM for DPP4 and EC50 of 30 nM for GPR119 transactivation activity. |
DC73442 |
AS1907417
|
AS1907417 is a potent, selective GPR119 agonist with cAMP EC50 of 1.1 uM (human GPR119). |
DC73441 |
AS1535907
|
AS1535907 is a potent GPR119 agonist with EC50 of 4.8 uM in HEK293 cells stably expressing human GPR119. |
DC70338 |
DA-1241
|
DA-1241 (DA1241) is a novel potent, highly selective GPR119 agonist, activates human GPR119 (EC50=4.37 nM) in increasing cAMP levels in GPR119-overexpressing HEK293 cells.DA-1241 increased cAMP levels via activated mouse GPR119 (EC50, 71.5 nM) and rat GPR119 (EC50, 156 nM).DA-1241 showed no significant activity against 156 off-target proteins at 10 uM, including human GLP-1 receptor and human GPR40.DA-1241 stimulated insulin secretion in hamster insulinoma HIT-T15 cells with EC50 of 22.3 nM, association with enhanced human insulin promoter activity.DA-1241 significantly reduced postprandial glucose excursion, significantly preserved β-cell mass with reduced PDX1 levels in the islets from HFD/STZ diabetic mice.DA-1241 reduced triglyceride content in the liver thereby improved fatty liver, reduced gluconeogenic enzyme expression in HepG2 cells and mouse liver, reduced autophagic flow in HepG2 cells. |
DC70139 |
GSK 2041706
|
A potent, selective and orally bioavailable GPR119 agonist with EC50 of 4 nM, with good selectivity versus a battery of receptors, ion channels and enzymes; causes greater reductions in cumulative food intake and higher fed plasma GLP-1 and peptide tyrosine tyrosine levels and decreased plasma insulin and glucose-dependent insulinotropic polypeptide levels, when combined with metformin, in diet-induced obese mice. |