Cantharidic Acid (sodium salt) |
| Catalog No.GC12082 |
PP1 and PP2A inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1465-77-6
Sample solution is provided at 25 µL, 10mM.
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Cantharidic acid, an inhibitor of protein phosphatases, is first isolated from Chinese blister beetles. Cantharidic acid is a hydrolysis product of cantharidin.
Protein phosphatases, account for virtually all of the phosphatase activity toward phosphoproteins, have been involved in controlling glycogen metabolism, glycolysis, gluconeogenesis, fatty acid synthesis, cholesterol synthesis, and protein synthesis. Protein phosphatases participate in protein phosphorylation, a principal regulatory mechanism in the control of almost all cellular processes [2].
In vitro: Cantharidic acid exihibited inhibitory effects on the protein phosphatases PP1 and PP2A with IC50 values of 0.6 and 0.05 μM, respectively. Cantharidic acid showed no effect on the activity of PP2B or PP2C [1].
In vivo: Intraperitoneal administration of cantharidic acid (10 mg/kg) to mice for 45 min caused extreme liver enlargement and congestion. Treatment with cantharidic acid increased hepatic glycogenolysis, elevated blood glucose and hepatic glycogen phosphorylase levels, reduced hepatic glycogen content and glycogen synthase activity. Cantharidic acid endothal decreased microsomal Mg2+-ATPase levels [3].
References:
[1] McCluskey A, Sim A T R, Sakoff J A. Serine threonine protein phosphatase inhibitors: Development of potential therapeutic strategies[J]. Journal of medicinal chemistry, 2002, 45(6): 1151-1175.
[2] Ingebritsen T S, Cohen P. Protein phosphatases: properties and role in cellular regulation[J]. Science, 1983, 221(4608): 331-338.
[3] Graziano M J, Casida J E. Comparison of the acute toxicity of endothal and cantharidic acid on mouse liver in vivo[J]. Toxicology letters, 1987, 37(2): 143-148.
| Cas No. | 1465-77-6 | SDF | |
| Chemical Name | (1R,2S,3R,4S)-rel-2,3-dimethyl-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid, disodium salt | ||
| Canonical SMILES | OC([C@@]1(C)[C@](C(O)=O)(C)[C@@H]2CC[C@H]1O2)=O.[Na+].[Na+] | ||
| Formula | C10H12O5 • 2Na | M.Wt | 258.2 |
| Solubility | ≤2mg/ml in PBS(pH7.2) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.873 mL | 19.3648 mL | 38.7297 mL |
| 5 mM | 0.7746 mL | 3.873 mL | 7.7459 mL |
| 10 mM | 0.3873 mL | 1.9365 mL | 3.873 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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