SML1883
AR231453
≥98% (HPLC)
别名:
AR231453, (2-Fluoro-4-methanesulfonylphenyl)-(6-[4-(3-isopropyl-[1,2,4]oxadiazol-5-yl)-piperidin-1-yl]-5-nitropyrimidin-4-yl)amine, AR-231,453, N-(2-Fluoro-4-(methylsulfonyl)phenyl)-6-(4-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl)-5-nitropyrimidin-4-amine
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选择尺寸
关于此项目
经验公式（希尔记法）:
C21H24FN7O5S
化学文摘社编号:
分子量:
505.52
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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)
SMILES string
CC(C)C1=NOC(C(CC2)CCN2C(N=CN=C3NC4=CC=C(C=C4F)S(=O)(C)=O)=C3[N+]([O-])=O)=N1
InChI key
DGBKNTVAKIFYNU-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
AR231453 is a 5-nitropyrimidine derivative that acts as a highly potent and selective GPR119 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.
An orally active, highly potent and selective GRP119 agonist with in vivo efficacy in improving glucose tolerance in mice and rats.
存储类别
11 - Combustible Solids
wgk
WGK 3
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
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
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
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