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  2. Biochemical Assay Reagents
  3. CP-91149

CP-91149 是 GP (糖原磷酸化酶) 的抑制劑。CP-91149 促進(jìn)糖原的重新合成,但不導(dǎo)致糖原的過(guò)度積累。CP-91149 有用于2型糖尿病研究的潛能。

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CP-91149 Chemical Structure

CP-91149 Chemical Structure

CAS No. : 186392-40-5

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10 mM * 1 mL in DMSO ¥440
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1 mg ¥233
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5 mg ¥500
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10 mg ¥750
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25 mg ¥1350
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50 mg ¥2025
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100 mg ¥3000
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)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]
體外研究
(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

399.88

Formula

C21H22ClN3O3

CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (250.08 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5008 mL 12.5038 mL 25.0076 mL
5 mM 0.5002 mL 2.5008 mL 5.0015 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

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

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.80%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5008 mL 12.5038 mL 25.0076 mL 62.5191 mL
5 mM 0.5002 mL 2.5008 mL 5.0015 mL 12.5038 mL
10 mM 0.2501 mL 1.2504 mL 2.5008 mL 6.2519 mL
15 mM 0.1667 mL 0.8336 mL 1.6672 mL 4.1679 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
Help & FAQs
  • 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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產(chǎn)品名稱:
CP-91149
目錄號(hào):
HY-13525
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