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MBX-2982

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Chemical Structure| 1037792-44-1 同义名 : -
CAS号 : 1037792-44-1
货号 : A882623
分子式 : C22H24N8OS
纯度 : 98%+
分子量 : 448.544
MDL号 : MFCD22628771
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(111.47 mM)，配合低频超声助溶，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
动物实验配方：
生物活性
描述 G protein-coupled receptor 119 (GPR119), a class A G protein-coupled receptor (GPCR), is involved in regulating metabolic homoeostasis, with GPR119 agonists targeted for the treatment of type-2 diabetes and obesity. MBX-2982 is a selective, orally-available GPR119 agonist. In cells pretreated with MBX-2982 (1 μM) in “chronic incubation/washout” experiments, cAMP accumulation was significantly increased compared to control cells and the sustained response after “chronic incubation/washout” was high at 84.62 ± 20.22% of acute response. In GLUTag cells, MBX-2982 (1 μM; 120 min) evoked a statistically significant increase in GLP-1 secretion compared to control cells[3]. In C57BL/6 mice, MBX-2982 at a dose of 10 mg/kg increased the plasma GLP-1 levels without a glucose load[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.15mL

2.23mL

1.11mL

22.29mL

4.46mL

2.23mL
参考文献

[1]Hothersall JD, Bussey CE, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42.

[2]Lan H, Lin HV, et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br J Pharmacol. 2012 Apr;165(8):2799-807.

[3]Hothersall JD, Bussey CE, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42

[4]Lan H, Lin HV, et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br J Pharmacol. 2012 Apr;165(8):2799-807