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CP-91149 是 GP (糖原磷酸化酶) 的抑制剂。CP-91149 促进糖原的重新合成,但不导致糖原的过度积累。CP-91149 有用于2型糖尿病研究的潜能。

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CP-91149 Chemical Structure

CP-91149 Chemical Structure

CAS No. : 186392-40-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CP-91149 is a GP (glycogen phosphorylase) inhibitor. CP-91149 promotes glycogen resynthesis, but not its overaccumulation. CP-91149 has the potential for Type II (insulin-dependent) diabetes study[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Hepatocyte IC50
3172.5 nM
Compound: CP-91149
Inhibition of glycogenolysis in rat hepatocytes assessed as GCN-stimulated glycogen breakdown after 5 mins
Inhibition of glycogenolysis in rat hepatocytes assessed as GCN-stimulated glycogen breakdown after 5 mins
[PMID: 32527535]
HepG2 IC50
3310.4 nM
Compound: CP-91149
Inhibition of glycogenolysis in human HepG2 cells assessed as GCN-stimulated glycogen breakdown after 5 mins
Inhibition of glycogenolysis in human HepG2 cells assessed as GCN-stimulated glycogen breakdown after 5 mins
[PMID: 32527535]
Sf9 IC50
0.082 μM
Compound: D; CP-91149
Inhibition of human recombinant liver glycogen phosphorylase A expressed in baculovirus infected Sf9 insect cells assessed as release of phosphate from glucose-1- phosphate in presence of 7.5 mM glucose by malachite green based assay
Inhibition of human recombinant liver glycogen phosphorylase A expressed in baculovirus infected Sf9 insect cells assessed as release of phosphate from glucose-1- phosphate in presence of 7.5 mM glucose by malachite green based assay
[PMID: 27624527]
Sf9 IC50
110 nM
Compound: CP-91149
Inhibition of recombinant human liver glycogen phosphorylase a expressed in baculovirus-infected Sf9 cells using glucose-1-phosphate as substrate in presence of 7.5 mM glucose
Inhibition of recombinant human liver glycogen phosphorylase a expressed in baculovirus-infected Sf9 cells using glucose-1-phosphate as substrate in presence of 7.5 mM glucose
[PMID: 32527535]
体外研究
(In Vitro)

CP-91149 treatment decreases muscle GP activity by converting the phosphorylated AMP-independent α form into the dephosphorylated AMP-dependent b form and inhibiting GP α activity and AMP-mediated GP b activation[1].
CP-91149 (10, 30, 50 μM) inhibits brain GP and causes glycogen accumulation in A549 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Cells were transduced with adenoviruses and incubated in the presence of 25 mM glucose for 2 days.
Concentration: 10 µM (glucose− or glucose+ for 18 h).
Incubation Time: 3 h.
Result: Promoted the conversion of GP a into GP b, according to α model proposed in hepatocytes.

Western Blot Analysis[2]

Cell Line: A549 cells.
Concentration: 0, 10, 30, 50 μM.
Incubation Time: 72 h.
Result: A significant increase in glycogen accumulation was detected at 10 μM of CP-91149 as compared with untreated cells with a maximal glycogen accumulation at 30 μM. Intracellular glycogen content decreased at 50 μM CP-91149, perhaps explained by additional pharmacological effects of the drug. The dose-dependent accumulation of intracellular glycogen in A549 cells by CP-91149 indicates that CP-91149 inhibits brain GP in tissue culture.
分子量

399.87

Formula

C21H22ClN3O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (250.08 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5008 mL 12.5041 mL 25.0081 mL
5 mM 0.5002 mL 2.5008 mL 5.0016 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.25 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.25 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.80%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5008 mL 12.5041 mL 25.0081 mL 62.5203 mL
5 mM 0.5002 mL 2.5008 mL 5.0016 mL 12.5041 mL
10 mM 0.2501 mL 1.2504 mL 2.5008 mL 6.2520 mL
15 mM 0.1667 mL 0.8336 mL 1.6672 mL 4.1680 mL
20 mM 0.1250 mL 0.6252 mL 1.2504 mL 3.1260 mL
25 mM 0.1000 mL 0.5002 mL 1.0003 mL 2.5008 mL
30 mM 0.0834 mL 0.4168 mL 0.8336 mL 2.0840 mL
40 mM 0.0625 mL 0.3126 mL 0.6252 mL 1.5630 mL
50 mM 0.0500 mL 0.2501 mL 0.5002 mL 1.2504 mL
60 mM 0.0417 mL 0.2084 mL 0.4168 mL 1.0420 mL
80 mM 0.0313 mL 0.1563 mL 0.3126 mL 0.7815 mL
100 mM 0.0250 mL 0.1250 mL 0.2501 mL 0.6252 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CP-91149
目录号:
HY-13525
需求量: