GPR120-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/GPR120.html GPR120G-protein coupled receptor 120GPR120 (Free fatty acid receptor 4, FFA4) is a G protein-coupled receptor that acts as a sensor of long-chain fatty acids, modulatesmetabolism, and whose dysfunction participates in endocrine disturbances. In huma

2、ns, two isoforms, long and short, of GPR120receptors have been reported. Human GPR120 receptors couples with Gq/11 and activates phospholipase C, leading to thehydrolysis of phosphatidylinositol 4, 5-bisphosphate, generating inositol trisphosphate and diacylglycerol. Inositol trisphosphatetriggers c

3、alcium release from intracellular stores, whereas diacylglycerol, together with calcium, activates protein kinase C.GPR120 has been shown to be densely expressed in human lungs and colon, as well as in adipocytes and macrophages, where itrecognizes long-chained FFAs including palmitic acid, oleic ac

4、id, myristic acid, and importantly, the family of polyunsaturatedomega-3 fatty acids, including -linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA). Agonism ofGPR120 has been shown to mediate endocrine processes including secretion of glucagon-like peptide-1 (GLP-1) an

5、dcholecystokinin from intestinal enteroendocrine cells, inhibition of ghrelin secretion from gastric ghrelin cells, and regulation ofadipocyte differentiation. GPR120 agonism has been shown to modulate numerous anti-inflammatory and insulin-sensitizingeffects including suppression of TNF- and IL-6 s

6、ecretion from macrophages and enhancement of GLUT4 translocation and glucoseuptake in adipocytes. GPR120 is a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM).www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/GPR120.html GPR120 HYPERLINK https:/www.MedChemE/

7、Targets/GPR120.html HYPERLINK https:/www.MedChemE/Targets/GPR120.html Agonists, HYPERLINK https:/www.MedChemE/Targets/GPR120.html HYPERLINK https:/www.MedChemE/Targets/GPR120.html Antagonists, HYPERLINK https:/www.MedChemE/Targets/GPR120.html HYPERLINK https:/www.MedChemE/Targets/GPR120.html Activat

8、ors HYPERLINK https:/www.MedChemE/Targets/GPR120.html HYPERLINK https:/www.MedChemE/Targets/GPR120.html & HYPERLINK https:/www.MedChemE/Targets/GPR120.html HYPERLINK https:/www.MedChemE/Targets/GPR120.html Modulators HYPERLINK https:/www.MedChemE/racemic-pinocembrin.html ()-Pinocembrin()-5,7-Dihydro

9、xyflavanone; NSC 43318) Cat. No.: HY-N2540 HYPERLINK https:/www.MedChemE/13z-16z-docosadienoic-acid.html 13Z,16Z-Docosadienoic HYPERLINK https:/www.MedChemE/13z-16z-docosadienoic-acid.html HYPERLINK https:/www.MedChemE/13z-16z-docosadienoic-acid.html acidCat. No.: HY-114610()-Pinocembrin ()-5,7-Dihy

10、droxyflavanone) is aGPR120 ligand able to promote wound healing inHaCaT cell line.13Z,16Z-Docosadienoic acid, a -6 polyunsaturatedfatty acid, possesses anti-borreliae effect.13Z,16Z-Docosadienoic acid, as a long-chain fattyacid (LCFA), is a free fatty acid receptor 4(FFAR4 or GPR120, a LCFA receptor

11、) agonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ah-7614.html AH-7614Cat. No.: HY-19996 HYPERLINK https:/www.MedChemE/Ginsenoside-Rb2.html Ginsenoside HYPERLINK https:/www.MedChe

12、mE/Ginsenoside-Rb2.html HYPERLINK https:/www.MedChemE/Ginsenoside-Rb2.html Rb2(Ginsenoside C) Cat. No.: HY-N0040AH-7614 is a potent and selective FFA4 (GPR120)antagonist, with pIC s of 7.1, 8.1, and 8.1 for50human, mouse, and rat FFA4, respectively. AH-7614has selectivity for FFA4 over FFA1 (pIC 98%

13、Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.07%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GPR120-IN-1.html GPR120 HYPERLINK https:/www.MedChemE/GPR120-IN-1.html HYPERLINK https:/www.MedChemE/GPR120-IN-1.html A

14、gonist HYPERLINK https:/www.MedChemE/GPR120-IN-1.html HYPERLINK https:/www.MedChemE/GPR120-IN-1.html 3 HYPERLINK https:/www.MedChemE/GPR120-IN-1.html HYPERLINK https:/www.MedChemE/gpr120-modulator-1.html GPR120 HYPERLINK https:/www.MedChemE/gpr120-modulator-1.html HYPERLINK https:/www.MedChemE/gpr12

15、0-modulator-1.html modulator HYPERLINK https:/www.MedChemE/gpr120-modulator-1.html HYPERLINK https:/www.MedChemE/gpr120-modulator-1.html 1Cat. No.: HY-101492 Cat. No.: HY-50162GPR120 Agonist 3 is a selective Gpr120 agonistwith a logEC of 7.62.50GPR120 modulator 1 is a G protein coupledreceptor 120 (

16、GPR120) modulator extracted frompatent US8394841B2, compound example F1. GPR120modulator 1 can be used for the research ofdiseases associated with abnormal or deregulatedGPR120, such as diabetes.Purity: 99.42%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPu

17、rity: 98.56%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/GPR120-modulator-2.html GPR120 HYPERLINK https:/www.MedChemE/GPR120-modulator-2.html HYPERLINK https:/www.MedChemE/GPR120-modulator-2.html modulator HYPERLINK https:/www.MedChemE/GPR1

18、20-modulator-2.html HYPERLINK https:/www.MedChemE/GPR120-modulator-2.html 2 HYPERLINK https:/www.MedChemE/GPR120-modulator-2.html HYPERLINK https:/www.MedChemE/grifolic-acid.html Grifolic HYPERLINK https:/www.MedChemE/grifolic-acid.html HYPERLINK https:/www.MedChemE/grifolic-acid.html acidCat. No.:

19、HY-50172 Cat. No.: HY-N3977GPR120 modulator 2 is a G protein coupledreceptor 120 (GPR120) modulator extracted frompatent US8394841B2, compound example F13. GPR120modulator 2 can be used for the research ofdiseases associated with abnormal or deregulatedGPR120, such as diabetes.Grifolic acid is a phe

20、nolic compound that is firstextracted from the mushroom Albatrellus confluens.Grifolic acid acts as an agonist of the free fattyacid receptor (FFAR4/GPR120).Purity: 97.25%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.0%Clinical Data: No Development ReportedSize

21、: 1 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/GSK137647A.html GSK137647A(GSK 137647) Cat. No.: HY-19995 HYPERLINK https:/www.MedChemE/medica16.html MEDICA16Cat. No.: HY-P1123GSK137647A is a selective FFA4 agonist, with pEC50of 6.3, 6.2, and 6.1 for human, Mouse and RatFFA4, respectively.MEDICA16, an ATP-citrate lyase inhi