CP-91149

價格	￥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: S2717	規(guī)格: 5mg/10mg/10mM/1mL/100mg

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

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

生物活性

產(chǎn)品描述	CP-91149在有葡萄糖存在時，選擇性抑制糖原磷酸化酶，IC50為0.13 μM，在無葡萄糖存在時，作用效果低5到10倍。
靶點(diǎn)	GP	?	?	?	?	?
IC50	0.13 μM ^[1]	?	?	?	?	?
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]

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.

細(xì)胞試驗(yàn): ^[3]

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

動物實(shí)驗(yàn): ^[1]

動物模型	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

公司簡介

成立日期		注冊資本
員工人數(shù)		年?duì)I業(yè)額
主營行業(yè)		經(jīng)營模式

Selleck中國

普通會員

公司成立：暫無
注冊資本：暫無
企業(yè)類型：暫無
主營產(chǎn)品：暫無
公司地址：

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CP-91149相關(guān)廠家報價

產(chǎn)品名稱	價格		公司名稱	報價日期
CP-91149	￥500		上海偉寰生物科技有限公司	2026-07-28
CP-91149	￥575.95		上海超研生物科技有限公司	2026-07-28
化合物 CP91149\|T6455\|TargetMol	￥186	VIP5年	TargetMol中國（陶術(shù)生物）	2026-06-29
aladdin 阿拉丁 C409278 CP-91149 186392-40-5 10mM in DMSO	￥635.90	VIP14年	上海阿拉丁生化科技股份有限公司	2026-06-23
aladdin 阿拉丁 E129719 CP-91149 186392-40-5 ≥99%	￥4706.90	VIP3年	上海阿拉丁生化科技股份有限公司	2026-06-10
CP-91149,186392-40-5	￥1572.07	VIP12年	西格瑪奧德里奇（上海）貿(mào)易有限公司	2023-10-27

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