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CP-91149
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CP-91149图片
CAS NO:186392-40-5
包装:10mg
包装与价格:
包装价格(元)
10mg电议

产品介绍

生物活性

CP-91149 is a human liver glycogen phosphorylase α (HLGPα) inhibitor with an IC50 of 0.13 μM in the presence of 7.5 mM glucose. CP-91149 suppressed glucagon-triggered glycogenolysis in isolated rat hepatocytes and in primary human hepatocytes. In vivo, oral injection of CP-91149 to diabetic ob/ob mice at 25–50 mg/kg led in rapid (3 h) glucose lowering by 100–120 mg/dl without producing hypoglycemia. In addition, upon treatment with CP-91149, A549 non-small cell lung carcinoma (NSCLC) cells accumulated glycogen with associated growth retardation. Treated normal skin fibroblasts also accumulated glycogen with G1-cell cycle arrest that was associated with inhibition of cyclin E-CDK2 activity. Overall, cells expressing high levels of brain GP were growth prevented by CP-91149 associating with glycogen accumulation whereas cells expressing low levels of brain GP were not affected by the agent.


化学数据

分子量399.87
分子式C21H22ClN3O3
CAS号186392-40-5
纯度>98%
溶解性(25°C)DMSO 70 mg/mL
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系HSF55 and T98G
方法Exposing cells to various concentrations of CP-91149 for 72hours. Determining viability with manual cell counts following staining with trypan blue exclusion assay. Fixing cells with 70% ethanol. Staining DNA with propidium iodide and the intensity of fluorescence is measured using a Becton-Dickinson flow cytometer at 488nm for excitation and at 650nm for emission. Using Modifit's Sync Wizard is analyze the cell cycle profile .
浓度Dissolved in DMSO, final concentrations ~50 μM
处理时间72 hours

动物实验
动物模型Obese, diabetic male C57BL/6J-Lep(ob/ob) mice and their lean, nondiabetic C57BL/6J-/+ littermates
配制Formulated in vehicle consisting of either 0.25% (wt/vol) methyl cellulose in water or 0.1% Pluronic P105 Block Copolymer Surfactant in 0.1% saline
剂量~50 mg/kg
给药处理Orally

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.5008 mL12.5041 mL25.0081 mL
5 mM0.5002 mL2.5008 mL5.0016 mL
10 mM0.2501 mL1.2504 mL2.5008 mL