AS1949490

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AS1949490 通过上调 L6 肌管中的 GLUT1 基因来激活葡萄糖代谢。

AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes. AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM.

Western Blot Analysis Cell Line:L6 myotubes Concentration:0, 4, 8, and 16 μM; 1 nM (insulin)Incubation Time:15 minutes Result:Increased insulin-induced phosphorylation of Akt in a dose-dependent manner.Western Blot Analysis Cell Line:L6 myotubes Concentration:10 μM Incubation Time:48 hours Result:Increased GLUT1 but not GLUT4 mRNA expression in L6 myotubes.

Animal Model:Male C57BL/KsJ Jcl-dbm mice and db/+db mice Dosage:300 mg/kg Administration:Oral administration; twice daily, for 7 or 10 days Result:Decreased plasma glucose (23% reduction, relative to vehicle).Reduced fasting blood glucose (37% reduction, relative to vehicle) and the area under the blood glucose concentration time curve (AUC).Increased the phosphorylation of GSK3β in the liver without changing the overall levels of GSK3β protein.Animal Model:Male ICR mice (6 weeks of age)Dosage:300 mg/kg Administration:Oral administration; once, for 8 hours Result:Reduced an approximately 50% of both PEPCK and G6Pase mRNA levels.

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Metabolic Enzyme/Protease

Phosphatase

PDE3| PDE4

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1203680-76-5

371.88

C20H18ClNO2S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (134.45 mM)

C[C@H](NC(=O)c1sccc1OCc1ccc(Cl)cc1)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years