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SR-18292

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Chemical Structure| 2095432-55-4 同义名 : -
CAS号 : 2095432-55-4
货号 : A160003
分子式 : C23H30N2O2
纯度 : 99%+
分子量 : 366.497
MDL号 : MFCD31657330
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(286.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(272.85 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

生物活性
描述 Peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) is a key transcriptional coactivator in energy homeostasis that regulates fat and glucose metabolism. SR-18292 selectively increased PGC-1α acetylation at a concentration of 20µM. Treatment of primary hepatocytes with 20µM SR-18292 significantly reduced the ability of glucagon to stimulate the expression of the Pck1 and G6pc genes. SR-18292 at 20µM also significantly suppressed gluconeogenic gene and protein expression induced by ectopic expression of PGC-1α. In a dietary mouse model of type II diabetes mellitus, i.p. injection of SR-18292 at a dose of 45mg/kg for 4 days significantly decreased fasting blood glucose levels and hepatic expression of Pck1 compared with vehicle-treated controls. SR-18292 at the same dosage also significantly enhanced glucose tolerance and insulin sensitivity both in DIO mice and Lepob/ob mice[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.64mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL
参考文献

[1]Sharabi K, Lin H, et al. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017 Mar 23;169(1):148-160.e15.

[2]Sharabi K, Lin H, Tavares CDJ, et al. Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes. Cell. 2017;169(1):148-160.e15.