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CP-91149
  • CP-91149

CP-91149

價(jià)格 ￥575.95
包裝 1EA
最小起訂量 1EA
發(fā)貨地 其他
更新日期 2020-01-14

產(chǎn)品詳情

英文名稱:CP-91149
貨號(hào): S2717規(guī)格: 5mg/10mg/10mM/1mL/100mg
2020-01-14 CP-91149 CP-91149 1EA/575.95RMB 575.95

Selleck Chemicals美國(guó)品牌，中國(guó)庫(kù)存現(xiàn)貨，Phosphorylase抑制劑，CAS#186392-40-5。
更多詳情請(qǐng)?jiān)L問中國(guó)唯一官方網(wǎng)站：

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



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生物活性

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產(chǎn)品描述 CP-91149在有葡萄糖存在時(shí)，選擇性抑制糖原磷酸化酶，IC50為0.13 μM，在無(wú)葡萄糖存在時(shí)，作用效果低5到10倍。
靶點(diǎn) GP ? ? ? ? ?
IC50 0.13 μM

[1]

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體外研究 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]
體內(nèi)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]
臨床實(shí)驗(yàn) ?
特征 ?

推薦的實(shí)驗(yàn)操作(此推薦來自于公開的文獻(xiàn)所以Selleck并不保證其有效性)

激酶實(shí)驗(yàn):

[1]

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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.

細(xì)胞試驗(yàn):

[3]

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細(xì)胞系 HSF55 and T98G
濃度 Dissolved in DMSO, final concentrations ~50 μM
處理時(shí)間 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.

動(dòng)物實(shí)驗(yàn):

[1]

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動(dòng)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
劑量 ~50 mg/kg
給藥處理 Orally?
溫馨提示：不可用于臨床治療。
關(guān)鍵字： CP-91149;化學(xué)試劑

公司簡(jiǎn)介

成立日期 注冊(cè)資本
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  • Selleck中國(guó)
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  • 注冊(cè)資本：暫無(wú)
  • 企業(yè)類型：暫無(wú)
  • 主營(yíng)產(chǎn)品：暫無(wú)
  • 公司地址：
詢盤

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