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Table 2 GPR119 synthetic agonists

From: Targeting the GPR119/incretin axis: a promising new therapy for metabolic-associated fatty liver disease

Name Chemical structure EC50 (μM) Pharmacological effects in vivo and in vitro Refs.
AR231453 0.0047–0.009 AR231453 increases the levels of cAMP, GLP-1, and insulin [68, 71, 72]
PSN821 Structure not disclosed NA PSN821 can reduce weight and increase GLP-1 levels [79, 122]
MBX-2982 0.0039 MBX-2982 increases GLP-1 secretion, improves blood glucose control, inhibits fat production and reduces cholesterol [123, 124]
GSK1292263 NA GSK1292263 reduces HbA1c levels and glucose excursion [123, 125]
LEZ763 Structure not disclosed NA NA [79]
JNJ-38431055 0.046 JNJ-38431055 reduces glucose excursion [55, 76]
DS-8500a 0.0515 DS-8500a improves abnormal glucose intolerance, increases GLP-1, insulin secretion and high-density lipoprotein cholesterol concentrations, reduces total cholesterol, low-density lipoprotein cholesterol and triglyceride concentrations [126,127,128,129,130,131,132]
ZYG-19 Structure not disclosed NA NA [79]
AR246881 0.0097 NA [76]
BMS-903452 0.014 BMS-903452 reduces glucose excursion, increases GLP-1 and insulin secretion [79]
AR44006 Structure not disclosed 0.1704 AR44006 increases insulin secretion [63]
AR435707 Structure not disclosed 0.0277 AR435707 increases insulin secretion [63]
GSK-1104252A 0.05 NA [79]
APD668 0.0027 APD668 reduces cholesterol, TG levels, body weight ALT and AST [55]
ARN-II NA ARN-II enhances GLP-1 secretion, increases cAMP level [133]
AZ1 NA AZ1 enhances GLP-1 secretion, increases cAMP level [133]
AZ2 NA AZ2 enhances GLP-1 secretion, increases cAMP level [133]
AZ3 NA AZ3 enhances GLP-1 secretion, increases cAMP level [133]
AS1269574 2.5 AS1269574 protects β cell function and alleviates disorders of glucose and lipid metabolism [134]
AS1535907 1.5–4.8 AS1535907 protects β cell function and promotes insulin secretion [135,136,137]
AS1907417 1.1 AS1907417 enhances intracellular cAMP, GSIS, and human insulin promoter activity and regulates adipogenesis [91]
AS1669058 0.11 AS1669058 improves glucose tolerance and promotes insulin secretion [79]
PSN119-2 0.4 NA [76, 79]
PSN632408 1.9 PSN632408 could increase the cAMP level and insulin secretion [138]
PSN375963 8.4 PSN375963 increases insulin and GLP-1 secretion [40]
PSN119-1 0.5 PSN119-1 increases insulin and GLP-1 secretion [139]
PSN119-1 M 0.2 PSN119-1 M increases insulin and GLP-1 secretion [139]
Compound 3 1.7 Compound 3 increases insulin and GLP-1 secretion [139]
Compound 1 0.5 Compound 1 increases insulin and GLP-1 secretion [139]
HD0471953 Structure not disclosed NA HD0471953 can improve glucose tolerance and increase cAMP level [83]
HD044703 structure not disclosed 0.11 HD044703 can improve glucose tolerance and enhance cAMP, GLP-1 and insulin secretion [140]
HD0471042 Structure not disclosed 0.65–0.85 HD0471042 can improve glucose tolerance and enhance cAMP, GLP-1 and insulin secretion [141]
ZB-16 0.00725 ZB-16 enhances GLP-1 and insulin secretion, decreases blood glucose levels and improves glucose utilization [142]
HBK001 0.03 HBK001 promotes the release of GLP-1, improves glucose tolerance and protects islet β cell function [90]
compound 8 0.013 Compound 8 reduces the level of blood glucose [143]
  1. NA not applicable
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Cellular & Molecular Biology Letters

ISSN: 1689-1392

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