| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
PP2A/protein phosphatase 2; PP1
|
|---|---|
| ln Vitro |
Cantharidic acid (0-20 μM; 24 h) significantly reduced cell viability, as revealed by upregulation of caspase activation in both extrinsic and intrinsic apoptotic pathways, as well as upregulation of ERK1/2, p38, and JNK1/2 pathways [1].
|
| ln Vivo |
Cantharidic acid (10 mg/kg; intraperitoneal injection; single injection) causes extreme liver enlargement and congestion in mice. Increased hepatic glycogenolysis is evidenced by increased blood glucose and glycogen phosphorylase levels and a corresponding decrease in hepatic glycogen content and glycogen synthase activity [3].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HONE-1, NPC-39, and NPC-BM Concentration: 0, 2.5 μM, 5 μM, 10 μM, or 20 μM Incubation Duration: 24 h Experimental Results: Markedly reduced cell viability. |
| Animal Protocol |
Endothal and cantharidic acid were administered intraperitoneally to mice at 75 and 10 mg/kg, respectively, to compare their acute toxicity on liver tissue in vivo. Within 45 min both treatments caused extreme liver enlargement and congestion. Hepatic glycogenolysis was increased as evidenced by elevations in blood glucose and hepatic glycogen phosphorylase levels and by corresponding reductions in hepatic glycogen content and glycogen synthase activity. Endothal decreased hepatic ATP concentrations, although neither compound altered mitochondrial Mg2+-ATPase activity. Microsomal Mg2+-ATPase levels, however, were reduced by both treatments. There were no indications that reactive intermediates were involved in the toxicity of either compound. The results show that endothal and cantharidic acid act directly and cause similar biochemical changes in mouse liver in vivo.[3]
|
| References |
[2]. Serine-threonine protein phosphatase inhibitors: development of potential therapeutic strategies. J Med Chem. 2002 Mar 14;45(6):1151-75.
[3]. Comparison of the acute toxicity of endothal and cantharidic acid on mouse liver in vivo. Toxicol Lett. 1987 Jul;37(2):143-8. |
| Additional Infomation |
Cantharidic acid is a monoterpenoid with an epoxy-bridged bicyclic dicarboxylic acid structure, which acts as an inhibitor of protein phosphatases 1 and 2A. It has a role as an EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor, a hepatotoxic agent and an apoptosis inducer. It is a monoterpenoid, a dicarboxylic acid, a bridged compound and an oxabicycloalkane. It is functionally related to a cantharidin.
|
| Molecular Formula |
C10H14O5
|
|---|---|
| Molecular Weight |
214.22
|
| Exact Mass |
186.053
|
| CAS # |
28874-45-5
|
| Related CAS # |
1465-77-6 (sodium); 56-25-7 (lactone); 76970-77-9 (imide)
|
| PubChem CID |
121475
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.359g/cm3
|
| Boiling Point |
407.8ºC at 760mmHg
|
| Flash Point |
164.1ºC
|
| Vapour Pressure |
8.62E-08mmHg at 25°C
|
| Index of Refraction |
1.531
|
| LogP |
0.3
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
15
|
| Complexity |
307
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
OC([C@]1([C@@H]2CC[C@@H](O2)[C@@]1(C)C(=O)O)C)=O
|
| InChi Key |
NMTNUQBORQILRK-XCVPVQRUSA-N
|
| InChi Code |
InChI=1S/C10H14O5/c1-9(7(11)12)5-3-4-6(15-5)10(9,2)8(13)14/h5-6H,3-4H2,1-2H3,(H,11,12)(H,13,14)/t5-,6+,9+,10-
|
| Chemical Name |
(1S,2R,3S,4R)-2,3-dimethyl-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid
|
| Synonyms |
cantharidic acid; 28874-45-5; (1r,2s,3r,4s)-2,3-Dimethyl-7-Oxabicyclo[2.2.1]heptane-2,3-Dicarboxylic Acid; CHEBI:78695; 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid, 2,3-dimethyl-, (1R,2S,3R,4S)-rel-; 2,3-dimethyl-7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid; Cantharidic Acid (sodium salt); Lopac-C-8088;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6681 mL | 23.3405 mL | 46.6810 mL | |
| 5 mM | 0.9336 mL | 4.6681 mL | 9.3362 mL | |
| 10 mM | 0.4668 mL | 2.3340 mL | 4.6681 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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