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AB141627

AR 231453, GPR119 agonist

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(2 Publications)

MW 505.5 Da, Purity >99%. Potent, selective G-protein coupled receptor 119 (GPR119) agonist (EC50 = 0.68 nM). Enhances glucose-induced insulin release. Antidiabetic activity. Orally active in vivo.

View Alternative Names

G protein coupled receptor 2, G-protein coupled receptor 119, GP119_HUMAN, GPCR 2, GPR 119, Glucose-dependent insulinotropic receptor, HGPCR 2, MGC119957, Seven transmembrane helix receptor

1 Images
Chemical Structure - AR 231453, GPR119 agonist (AB141627)
  • Chemical Structure

Lab

Chemical Structure - AR 231453, GPR119 agonist (AB141627)

2D chemical structure image of ab141627, AR 231453, GPR119 agonist

Key facts

CAS number

733750-99-7

Purity

>99%

Form

Solid

form

Molecular weight

505.5 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>4</sub>FN<sub>7</sub>O<sub>5</sub>S

PubChem

24939268

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-nitropyrimidin-4-amine

Biological description

Potent, selective G-protein coupled receptor 119 (GPR119) agonist (EC50 = 0.68 nM). Enhances glucose-induced insulin release. Antidiabetic activity. Orally active in vivo.

Canonical smiles

CC(C)C1=NOC(=N1)C2CCN(CC2)C3=NC=NC(=C3[N+](=O)[O-])NC4=C(C=C(C=C4)S(=O)(=O)C)F

InChi

InChI=1S/C21H24FN7O5S/c1-12(2)18-26-21(34-27-18)13-6-8-28(9-7-13)20-17(29(30)31)19(23-11-24-20)25-16-5-4-14(10-15(16)22)35(3,32)33/h4-5,10-13H,6-9H2,1-3H3,(H,23,24,25)

InChiKey

DGBKNTVAKIFYNU-UHFFFAOYSA-N

IUPAC Name

N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine

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.

GPR119 also known as Glucose-dependent insulinotropic receptor is a G protein-coupled receptor (GPCR) that plays an essential role in metabolic regulation. With a mass of approximately 51 kDa it is expressed mainly in pancreatic beta cells and intestinal enteroendocrine cells. This receptor senses dietary lipids and promotes insulin secretion in response to meals. It also couples with G proteins to initiate intracellular signaling cascades important for energy homeostasis.
Biological function summary

GPR119 functions as a sensor of lipid-derived molecules often acting as an aryl agonist receptor. It is not part of a larger complex but can activate a series of downstream pathways upon ligand binding. When activated by endogenous and synthetic agonists GPR119 stimulates the release of incretin hormones such as GLP-1 and GIP. This hormone release enhances insulin response and promotes optimal glycemic control essential in maintaining blood glucose levels.

Pathways

GPR119 signaling pathway is integral in glucose metabolism and energy balance. It links to both the incretin hormone signaling pathway and the insulin signaling pathway. Upon activation it influences the levels of cAMP an important secondary messenger that modulates several downstream effects including the regulation of the insulin receptor. GPR119 interacts with other proteins such as adenylate cyclase affecting insulin secretion and lipid metabolism.

GPR119 has significant relevance to type 2 diabetes and obesity. Its role in glucose homeostasis and energy balance makes it a potential therapeutic target for these conditions. Researchers examine GPR119 agonists as possible treatments for enhancing insulin secretion and controlling body weight. The receptor is linked to related pathways integrating multiple metabolic signals including those mediated by GLP-1 an important hormone involved in energy regulation and glycemic control.

Product protocols

Publications (2)

Recent publications for all applications. Explore the full list and refine your search

Diabetes 66:1626-1635 PubMed28254842

2017

β-Cell Inactivation of Unmasks Incretin Dependence of GPR119-Mediated Glucoregulation.

Applications

Unspecified application

Species

Unspecified reactive species

Brandon L Panaro,Grace B Flock,Jonathan E Campbell,Jacqueline L Beaudry,Xiemin Cao,Daniel J Drucker

Scientific reports 6:32529 PubMed27581068

2016

A role of CB1R in inducing θ-rhythm coordination between the gustatory and gastrointestinal insula.

Applications

Unspecified application

Species

Unspecified reactive species

Youngnam Kang,Hajime Sato,Mitsuru Saito,Dong Xu Yin,Sook Kyung Park,Seog Bae Oh,Yong Chul Bae,Hiroki Toyoda
View all publications

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