Abcam, ab142091, TGR5 Receptor Agonist, TGR5 G-protein coupled receptor agonist

Size: 5mg
MW 361.2 Da, Purity >99%. Potent, selective TGR5 G-protein coupled receptor agonist (pEC 50 = 6.8). Increases glucagon-like peptide-1 (GLP-1) secretion from primary intestinal cells. Cell-permeable. Active in vivo .
Key facts
CAS number:1197300-24-5,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:361.2 Da,
Molecular formula:C18H14Cl2N2O2,
PubChem:44605616,
Nature:Synthetic,
Solubility:Soluble in ethanol to 100 mMSoluble in DMSO to 100 mM,
Biochemical name:TGR5 Receptor Agonist,
Biological description:Potent, selective TGR5 G-protein coupled receptor agonist (pEC50 = 6.8). Increases glucagon-like peptide-1 (GLP-1) secretion from primary intestinal cells. Cell-permeable. Active in vivo.,
Canonical smiles:CC1=C(C(=NO1)C2=CC=CC=C2Cl)C(=O)N(C)C3=CC=C(C=C3)Cl,
InChi:InChI=1S/C18H14Cl2N2O2/c1-11-16(17(21-24-11)14-5-3-4-6-15(14)20)18(23)22(2)13-9-7-12(19)8-10-13/h3-10H,1-2H3,
InChiKey:IGRCWJPBLWGNPX-UHFFFAOYSA-N,
IUPAC Name:3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-dimethyl-1,2-oxazole-4-carboxamide

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
GPCR TGR5 also known as G protein-coupled bile acid receptor 1 (GPBAR1) is a member of the GPCR superfamily. This receptor weighs approximately 35 kDa and is expressed in various tissues including liver intestine brown adipose tissue and macrophages. It functions as a membrane receptor that binds bile acids which activates downstream signaling pathways influencing metabolic processes.
Biological function summary
GPCR TGR5 plays a role in energy metabolism and the immune response. It does not form part of a larger receptor complex but interacts with different proteins to mediate its effects. Upon activation by bile acids TGR5 stimulates the production of cyclic AMP (cAMP) and regulates the release of various cytokines influencing metabolic rate and promoting anti-inflammatory effects.
Pathways
GPCR TGR5 links to the cAMP signaling pathway and plays a role in the brown adipose tissue activation pathway. It is closely related to proteins like adenylate cyclase which it activates to increase cAMP levels and potentially interacts with nuclear receptors modifying gene expression linked to energy homeostasis and inflammation control.
GPCR TGR5 associates with metabolic disorders such as obesity and type 2 diabetes. Its role in regulating energy expenditure makes it a target for combating obesity where it influences pathways involving protein partners like adenylate cyclase. Additionally its involvement in controlling inflammation connects it to diseases involving immune dysregulation offering potential pathways for therapeutic interventions.