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> CP-91149 [186392-40-5]

CP-91149 [186392-40-5]

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Referência HY-13525-10mg

Tamanho : 10mg

Marca : MedChemExpress

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Description

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].

Cellular Effect
Cell Line Type Value Description References
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]
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]
SK-HEP1 IC50
1.5 μM
Compound: CP-91149
Inhibitory concentration against human SK-Hep-1 cells (hepatoma cell line)
Inhibitory concentration against human SK-Hep-1 cells (hepatoma cell line)
[PMID: 15603973]
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]
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].

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

CP-91149 Related Antibodies

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.
Masse moléculaire

399.88

Formule

C21H22ClN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N1)=CC2=C1C=CC(Cl)=C2)N[C@@H](CC3=CC=CC=C3)[C@@H](O)C(N(C)C)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (250.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
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