SML1883

Sigma-Aldrich

AR231453

≥98% (HPLC)

Sinónimos:
AR231453, N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-nitropyrimidin-4-amine, AR-231,453, (2-Fluoro-4-methanesulfonylphenyl)-(6-4-(3-isopropyl-1,2,4oxadiazol-5-yl)-piperidin-1-yl-5-nitropyrimidin-4-yl)amine
Empirical Formula (Hill Notation):
C21H24FN7O5S
Número de CAS:
Peso molecular:
505.52
MDL number:
En este momento no podemos mostrarle ni los precios ni la disponibilidad

Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

−20°C

SMILES string

CC(C)C1=NOC(C(CC2)CCN2C(N=CN=C3NC4=CC=C(C=C4F)S(=O)(C)=O)=C3N+(O-)=O)=N1

Biochem/physiol Actions

AR231453 is a 5-nitropyrimidine derivative that acts as a highly potent and selective GRP119 agonist (EC50/GPR119 species = 0.4 nM/monkey, 1.6 nM/dog, 4.7 nM/hamster, 3.5 nM/human, 12 nM/mouse, 4 nM/rat in cell-based assays), exhibiting no off-target activity toward 216 receptors, enzymes, and orphan GPCRs. AR231453 improves glucose tolerance in mice (3 mg/kg i.p. or 20 mg/kg, p.o.) and rats (3 mg/kg i.p.), while no in vivo efficacy is observed among GPR119-deficient mice.

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point F

Not applicable

Flash Point C

Not applicable

Zhi-Liang Chu et al.
Endocrinology, 148(6), 2601-2609 (2007-02-10)
Pancreatic beta-cell dysfunction is a hallmark event in the pathogenesis of type 2 diabetes. Injectable peptide agonists of the glucagon-like peptide 1 (GLP-1) receptor have shown significant promise as antidiabetic agents by virtue of their ability to amplify glucose-dependent insulin...
Graeme Semple et al.
Journal of medicinal chemistry, 51(17), 5172-5175 (2008-08-14)
GPR119 is a rhodopsin-like GPCR expressed in pancreatic beta-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive potential target for the treatment of...
Christoffer Norn et al.
Structure (London, England : 1993), 23(12), 2377-2386 (2015-11-04)
Recent benchmark studies have demonstrated the difficulties in obtaining accurate predictions of ligand binding conformations to comparative models of G-protein-coupled receptors. We have developed a data-driven optimization protocol, which integrates mutational data and structural information from multiple X-ray receptor structures...
Deborah A Goldspink et al.
Cell reports, 31(13), 107833-107833 (2020-07-02)
Glucagon-like peptide-1 (GLP-1) from intestinal L-cells stimulates insulin secretion and reduces appetite after food ingestion, and it is the basis for drugs against type-2 diabetes and obesity. Drugs targeting L- and other enteroendocrine cells are under development, with the aim...

Nuestro equipo de científicos tiene experiencia en todas las áreas de investigación: Ciencias de la vida, Ciencia de los materiales, Síntesis química, Cromatografía, Analítica y muchas otras.

Póngase en contacto con el Servicio técnico

Redes sociales

LinkedIn icon
Twitter icon
Facebook Icon
Instagram Icon

Merck

Investigación. Desarrollo. Producción.

Somos un proveedor líder para la industria de Ciencias de la Vida con soluciones y servicios para investigación, desarrollo y producción biotecnológicos, y para desarrollo y producción de tratamientos farmacéuticos

© 2021 Merck KGaA, Darmstadt, Alemania y/o sus filiales. Todos los derechos reservados.

Queda estrictamente prohibida la reproducción sin permiso de cualquiera de los materiales de la página web.