Table 2 GPR119 synthetic agonists

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]