CP-91149

价格	￥575.95
包装	1EA

最小起订量	1EA
发货地	其他
更新日期	2020-01-14

产品详情

英文名称:CP-91149
货号: S2717	规格: 5mg/10mg/10mM/1mL/100mg

Selleck Chemicals美国品牌，中国库存现货，Phosphorylase抑制剂，CAS#186392-40-5。
更多详情请访问中国唯一官方网站：

http://www.selleck.cn/products/cp-91149.html

生物活性

产品描述	CP-91149在有葡萄糖存在时，选择性抑制糖原磷酸化酶，IC50为0.13 μM，在无葡萄糖存在时，作用效果低5到10倍。
靶点	GP
IC50	0.13 μM ^[1]
体外研究	CP-91149 displays 200-fold higher inhibitory activity against human liver glycogen phosphorylase a (HLGPa) than caffeine (IC50 = 26 μM). CP-91149 (10-100 μM) inhibits glucagon-stimulated glycogenolysis in isolated rat hepatocytes in a dose-dependent manner, and in primary human hepatocytes with IC50 of ~2.1 μM. ^[1] CP-91149 also potently inhibits the activities of human muscle phosphorylase a and b with IC50 of 0.2 μM and ~0.3 μM, respectively. CP-91149 treatment at 2.5 μM induces inactivation of phosphorylase and sequential activation of glycogen synthase in hepatocytes, and increases glycogen synthesis by 7-fold at 5 mM glucose and by 2-fold at 20 mM glucose. CP-91149 can partially counteract the effects of phosphorylase overexpression. ^[2] CP-91149 also potently inhibits brain GP with IC50 of 0.5 μM in A549 cells. CP-91149 treatment at 10-30 μM causes significant glycogen accumulation in A549 and HSF55 cells. CP-91149 treatment increases G1-phase cells with a significant reduction of the S-phase population in HSF55 cells, correlated with increased expression of p21 and p27. ^[3] CP-91149 also promotes the dephosphorylation and activation of GS (glycogen synthase) in non-engineered or GP-overexpressing cultured human muscle cells, but exclusively in glucose-deprived cells. ^[4]
体内研究	Oral administration of CP-91149 to diabetic ob/ob mice at 25-50 mg/kg causes rapid (3 hours) glucose lowering by 100-120 mg/dl without producing hypoglycemia, resulting from inhibition of glycogenolysis in vivo. CP-91149 treatment does not lower glucose levels in normoglycemic, nondiabetic mice. ^[1] In the non-fasted Goto-Kakizaki (GK) rats, administration of CP-91149 in combination with CS-917 suppresses hepatic glycogen reduction by CS-917 and decreases plasma glucose more than single administration of CS-917. ^[5]
临床实验
特征

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验: ^[1]

Phosphorylase enzyme assay	Human liver glycogen phosphorylase a (HLGPa, 85 ng) activity is measured in the direction of glycogen synthesis by the release of phosphate from glucose-1-phosphate at 22°C in 100 μL of buffer containing 50 mM Hepes (pH 7.2), 100 mM KCl, 2.5 mM EGTA, 2.5 mM MgCl₂, 0.5 mM glucose-1-phosphate, and 1 mg/mL glycogen. Phosphate is measured at 620 nm, 20 minutes after the addition of 150 μL of 1 M HCl containing 10 mg/mL ammonium molybdate and 0.38 mg/mL malachite green. Increasing concentrations of CP-91149 are added to the assay in 5 μL of 14% DMSO.

Phosphorylase enzyme assay

Human liver glycogen phosphorylase a (HLGPa, 85 ng) activity is measured in the direction of glycogen synthesis by the release of phosphate from glucose-1-phosphate at 22°C in 100 μL of buffer containing 50 mM Hepes (pH 7.2), 100 mM KCl, 2.5 mM EGTA, 2.5 mM MgCl₂, 0.5 mM glucose-1-phosphate, and 1 mg/mL glycogen. Phosphate is measured at 620 nm, 20 minutes after the addition of 150 μL of 1 M HCl containing 10 mg/mL ammonium molybdate and 0.38 mg/mL malachite green. Increasing concentrations of CP-91149 are added to the assay in 5 μL of 14% DMSO.

细胞试验: ^[3]

细胞系	HSF55 and T98G
浓度	Dissolved in DMSO, final concentrations ~50 μM
处理时间	72 hours
方法	Cells are exposed to various concentrations of CP-91149 for 72hours. Viability is determined with manual cell counts following staining with trypan blue exclusion assay. Cells are fixed with 70% ethanol. DNA is stained 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. The cell cycle profile is analyzed using Modifit's Sync Wizard.

动物实验: ^[1]

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

温馨提示：不可用于临床治疗。

关键字： CP-91149;化学试剂

公司简介

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CP-91149相关厂家报价

产品名称	价格		公司名称	报价日期
CP-91149	￥575.95		上海超研生物科技有限公司	2024-07-20
aladdin 阿拉丁 C409278 CP-91149 186392-40-5 10mM in DMSO	￥635.90	VIP12年	上海阿拉丁生化科技股份有限公司	2024-06-14
aladdin 阿拉丁 E129719 CP-91149 186392-40-5 ≥99%	￥4706.90	VIP1年	上海阿拉丁生化科技股份有限公司	2024-06-03
CP-91149,186392-40-5	￥1572.07	VIP10年	西格玛奥德里奇（上海）贸易有限公司	2023-10-27
CP-91149	￥500		上海伟寰生物科技有限公司	2020-01-17

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