gpr120

GPR120 Agonist 2 is a potent and selective GPR120 receptor agonist.

GPR120 Agonist 1 is a selective GPR120 agonist. In GPR120 transfected HEK293 cells, GPR120 Agonist 1 displays good EC50 of 42 nM and 77 nM for human and mouse GPR120 (the calcium flux assay), respectively.

GPR120 modulator 1 is useful for modulating GPR120.

GPR120-IN-1 is a novel GPR120 inhibitor, showing ~90% inhibitory effects on cell growth with micromolar affinities against SW480.

GPR120 modulator 2 is useful for modulating GPR120.

GPR120 Agonist 3 (GPR120-IN-1) is a selective agonist of Gpr120 ( logEC50: -7.62).

Ginsenoside Rb2 (Ginsenoside C) found in species of Panax, upregulating GPR120 gene expression.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

GW9508(GW 9508) is a potent and selective agonist for FFA1 (GPR40), stimulates insulin secretion in a glucose-sensitive manner.

NCG21 is a GPR120 agonist, which showed potent extracellular signal-regulated kinase (ERK) activation in a cloned GPR120 system. NCG21 potently activated ERK, intracellular calcium responses and GLP-1 secretion in murine enteroendocrine STC-1 cells that e

(+/-)-Pinocembrin (NSC-43318), a natural product from axillary pines, is a GPR120 ligand that promotes wound healing in the HaCaT cell line.

TUG-905 is an agonist for free fatty acid receptor 4 (FFA4/GPR120), and TUG-905 has the potential to treat agitation.

AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist.

Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 |Zhang et al (2016) Discovery and characterization of a novel small-molecule agonist for medium-chain free fatty acid receptor G protein-coupled receptor 84. J.Pharmacol.Exp.Ther. 357 337 PMID:26962172

AMG 837 calcium hydrate is a potent GPR40 agonist with an EC50 of 13 nM. AMG 837 calcium hydrate also shows highly selective over GPR41, GPR43, and GPR120 (EC50 > 10,000 nM).

TUG-891 is a G protein-coupled receptor (GPCR) expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids.

1,1'-(Azodicarbonyl)dipiperidine (ADDP) serves as a widely employed reagent in the Mitsunobu reaction, facilitating the condensation between an alcohol and an acidic compound. Moreover, ADDP has found application in synthesizing agonists for the G protein-coupled receptor 120 (GPR120) with potential antidiabetic effects as well as in the creation of triple agonists for peroxisome proliferator-activated receptor α (PPARα), PPARγ, and PPARδ.

Metabolex-36 is a selective GPR120 agonist