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CP-91149

现货
Catalog No.
A8403
糖原磷酸化酶选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
Ship with 10-15 days
100mg
¥ 2,590.00
Ship with 10-15 days
5mg
¥ 500.00
Ship with 10-15 days
10mg
¥ 800.00
Ship with 10-15 days

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Background

CP-91149 is a selective inhibitor of glycogen phosphorylase (GP) with an IC50 value of 0.13 μM.

Glycogen phosphorylase is a phosphorylase enzymes that can catalize phosphorolytic cleavage of the glycosidic linkages of glycogen by releasing glucose-1-phosphate from the terminal alpha-1, 4-glycosidic bond. It controls the rate-limiting step in glycogenolysis in the cells.

In vitro, CP-91149 treatment suppressed glycogenolysis stimulated by glucagon in in primary human hepatocytes and isolated rat hepatocytes with IC50 value of 2.1 μM and 10–100 μM, respectively 1. Inhibition of phosphorylase a by CP-91149 resulted in activation of glycogen synthase and translocation of the protein from a soluble to a particulate fraction, which mimicked the insulin- stimulated glycogen synthesis 2.

In vivo, treatment of CP-91149 on diabetic ob/ob mice at a dosage of 25–50 mg/kg was shown to lead to a rapid glucose lowering but did not change glucose levels in normoglycemic, nondiabetic mice 1.

References:
1.  Martin WH, Hoover DJ, Armento SJ, et al. Discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in vivo. Proceedings of the National Academy of Sciences of the United States of America. 1998;95(4):1776-1781.
2.  Aiston S, Coghlan MP, Agius L. Inactivation of phosphorylase is a major component of the mechanism by which insulin stimulates hepatic glycogen synthesis. European journal of biochemistry / FEBS. 2003;270(13):2773-2781.

文献引用

1. Barot S, Abo-Ali EM, et al. "Inhibition of glycogen catabolism induces intrinsic apoptosis and augments multikinase inhibitors in hepatocellular carcinoma cells." Exp Cell Res. 2019 Aug 15;381(2):288-300. PMID:31128107

Chemical Properties

StorageStore at -20°C
M.Wt399.87
Cas No.186392-40-5
FormulaC21H22ClN3O3
Solubility≥16.4mg/mL in DMSO
Chemical Name5-chloro-N-[(2S,3R)-4-(dimethylamino)-3-hydroxy-4-oxo-1-phenylbutan-2-yl]-1H-indole-2-carboxamide
SDFDownload SDF
Canonical SMILESCN(C)C(=O)C(C(CC1=CC=CC=C1)NC(=O)C2=CC3=C(N2)C=CC(=C3)Cl)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

来源于雄性Wistar大鼠肝的肝脏细胞

溶解方法

在DMSO中的溶解度>16.4mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月

反应时间

2.5μm; 3h.

应用

在肝细胞中,CP-91149可以特异性抑制磷酸化酶,导致磷酸化酶由a到b的转变。CP-91149通过对磷酸化酶a的去磷酸化,而非抑制糖原降解或循环,从而刺激糖原合成。

动物实验[2]:

动物模型

雄性糖尿病C57BL/6J-Lep(ob/ob)小鼠

剂量

10、25、50 mg/kg(后两个浓度具有效应),口服

应用

在雄性糖尿病C57BL/6J-Lep(ob/ob)小鼠中,由CP-91149导致的葡萄糖降低具有统计学意义,在50 mg/kg使用浓度时小鼠达到了正常血糖。CP-91149可以抑制肝糖分解并降低血糖水平。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Aiston S, Coghlan MP, Agius L. Inactivation of phosphorylase is a major component of the mechanism by which insulin stimulates hepatic glycogen synthesis. European journal of biochemistry / FEBS. 2003;270(13):2773-2781.

[2] Martin WH, Hoover DJ, Armento SJ, et al. Discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in vivo. Proceedings of the National Academy of Sciences of the United States of America. 1998;95(4):1776-1781.

生物活性

Description CP-91149是糖原磷酸化酶(GP)的选择性抑制剂,其IC50值为0.13 μM。
靶点 GP          
IC50 0.13 μM          

质量控制

质量控制和MSDS

批次:

化学结构

CP-91149

相关生物数据

CP-91149