产品
编 号:F069279
分子式:C20H18ClNO2S
分子量:371.88
产品类型
结构图
CAS No: 1203680-76-5
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产品详情
生物活性:
AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50, and >50 μM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes.
体内研究:
AS1949490 (300 mg/kg;口服;每天两次,持续 7 或 10 天) 降低糖尿病小鼠的血浆葡萄糖并激活细胞内胰岛素信号传导。AS1949490 (300 mg/kg;口服 一次,持续 8 h;雄性 ICR 小鼠) 抑制糖异生和相关基因的表达。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.
体外研究:
AS1949490 (0-16 μM;15 分钟;L6 肌管) 增加胰岛素诱导的 Akt 磷酸化。 AS1949490 (0-10 μM;48 小时) 激活葡萄糖代谢并刺激L6 肌管中的葡萄糖摄取活性。 AS1949490 (0-10 μM;24 小时;L6 肌管) 降低胰岛素诱导的糖异生水平。 AS1949490 (10 μM;48 小时) 通过上调 L6 肌管中的 GLUT1 基因激活葡萄糖代谢。