GPR119-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/GPR119.html GPR119G protein coupled receptor 119G protein-coupled receptor 119 (GPR119) is a member of the class A (rhodopsin-type) GPCR family, which is highly expressed ononly a limited number of tissues, such as pancreatic -cells and enteroendocrine cells of

2、 the gastrointestinal tract in humans. Theactivation of GPR119 has the stimulatory effects of glucose-dependent insulin secretion in pancreatic -cells as well as intestinalsecretion of incretin hormones including glucose-dependent insulinotropic peptide (GIP) and glucagon-likepeptide1 (GLP-1). Taken

3、together, these effects represented a potential mechanism for modulation of glucose homeostasis and an attractive approach tothe treatment of type 2 diabetes mellitus (T2DM). GPR119 can be activated by oleoylethanolamide and several other endogenouslipids containing oleic acid: these include N-oleoy

4、l-dopamine, 1-oleoyl-lysophosphatidylcholine, generated in the tissue, and2-oleoyl glycerol generated in the gut lumen.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/GPR119.html GPR119 HYPERLINK https:/www.MedChemE/Targets/GPR119.html HYPERLINK https:/www.MedChemE/Targets/GPR119.html Agonists

5、HYPERLINK https:/www.MedChemE/2-oleoylglycerol.html 2-OleoylglycerolCat. No.: HY-W011121 HYPERLINK https:/www.MedChemE/APD597.html APD597(JNJ-38431055) Cat. No.: HY-155662-Oleoylglycerol is a dietary naturally occurringlipid. 2-Oleoylglycerol is a GPR119 agonist, withan EC of 2.5 M for human GPR119

6、in50transiently transfected COS-7 cells.2-Oleoylglycerol stimulates glucagon-likepeptide-1 (GLP-1) secretion in vivo.APD597 is a GPR119 agonist intended for thetreatment of type 2 diabetes, with EC50 of 46 nMfor hGPR119. IC50 value: 46 nM (EC50) Target:hGPR119 The design and synthesis of a secondgen

7、eration GPR119-agonist clinical candidate forthe treatment of diabetes is described.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg (28 mM * 500 L in Ethanol)Purity: 99.97%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/APD668.html APD66

8、8 HYPERLINK https:/www.MedChemE/APD668.html HYPERLINK https:/www.MedChemE/AR-231453.html AR HYPERLINK https:/www.MedChemE/AR-231453.html HYPERLINK https:/www.MedChemE/AR-231453.html 231453Cat. No.: HY-15565 Cat. No.: HY-15564APD668 is a potent, selective and orally activeagonist of G-protein coupled

9、 receptor GPR119, withEC50s of 2.7 nM and 33 nM for hGPR119 andrGPR119, respectively.AR 231453 is a potent, specific and orallyavailable GPR119 agonist. AR 231453 can stimulate-cell replication and improve islet graftfunction s.Purity: 99.71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5

10、mg, 10 mg, 50 mg, 100 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/as1269574.html AS1269574 HYPERLINK https:/www.MedChemE/as1269574.html HYPERLINK https:/www.MedChemE/Firuglipel.html FiruglipelCat. No.: HY-107535 Cat. No.: HY-10903

11、2AS1269574 is a potent, orally available GPR119agonist, with an EC of 2.5 M in HEK293 cells50expressing human GPR119. AS1269574 activates TRPA1cation channels to stimulate glucagon-likepeptide-1 (GLP-1) secretion.Firuglipel (DS-8500a) is an orally available,potent and selective GPR119 agonist.Purity

12、: 98.76%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.21%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GSK1292263.html GSK1292263 HYPERLINK https:/www.MedChemE/GSK1292263.html HYPERLINK https:/www

13、.MedChemE/mbx-2982.html MBX-2982Cat. No.: HY-12066 Cat. No.: HY-15291GSK-1292263 is an orally available GPR119 agonistwith pEC s of 6.9 and 6.7 for human and rat50GPR119, respectively. GSK-1292263 can be used forthe research of type 2 diabetes mellitus (T2DM).MBX-2982 is a selective, orally-availabl

14、e Gprotein-coupled receptor 119 (GPR119) agonist.Purity: 99.71%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.54%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/psn-375963.html PSN HYPERLINK https:/www.MedChemE/psn-375963

15、.html HYPERLINK https:/www.MedChemE/psn-375963.html 375963 HYPERLINK https:/www.MedChemE/psn-375963.html HYPERLINK https:/www.MedChemE/psn-375963-hydrochloride.html PSN HYPERLINK https:/www.MedChemE/psn-375963-hydrochloride.html HYPERLINK https:/www.MedChemE/psn-375963-hydrochloride.html 375963 HYPE

16、RLINK https:/www.MedChemE/psn-375963-hydrochloride.html HYPERLINK https:/www.MedChemE/psn-375963-hydrochloride.html hydrochlorideCat. No.: HY-108258 Cat. No.: HY-108258APSN 375963 is a potent GPR119 agonist, withEC s of 8.4 and 7.9 M for human and mouse50GPR119, respectively. PSN 375963 shows simila

17、rpotency to the endogenous agonistoleoylethanolamide (OEA).PSN 375963 hydrochloride is a potent GPR119agonist, with EC s of 8.4 and 7.9 M for human50and mouse GPR119, respectively. PSN 375963hydrochloride shows similar potency to theendogenous agonist oleoylethanolamide (OEA).Purity: 98.46%Clinical

18、Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/PSN632408.html PSN632408Cat. No.: HY-16673PSN632408, a selective, orally active GPR119agonist, shows si