| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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Purity: ≥98%
Dichloroacetate (CPC-211; DCA; X-11S) is a potent and specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively. It has the potential for the treatment of myocardia ischemia. Dichloroacetate has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth. DCA can trigger apoptosis of human lung, breast and brain cancer cells. After DCA treatment, cancer cells shows increased levels of ROS, depolarization of the MMP in vitro and increased apoptosis both in vitro and in vivo.
| ln Vitro |
In mitochondria, sodium dichloroacetate promotes the production of ROS. Sodium dichloroacetate influences cell viability and growth by increasing the production of reactive oxygen species (ROS) that arises from oxidative metabolism promotion. Pyruvate dehydrogenase kinases (PDK) inhibition, restored pyruvate dehydrogenase (PDH) activity, and the promotion of oxidative metabolism in conjunction with increased intracellular ROS production—all of which are dependent on the dosage of sodium dichloroacetate—were linked to the effects of sodium dichloroacetate on multiple myeloma cell viability, cell cycle arrest, and apoptotic cell death. In rat VM-M3 glioblastoma cells, the effects of sodium dichloroacetate combined with CI inhibition to promote oxidative stress. Elevated reactive oxygen species (ROS) in cancer cells treated with sodium dichloroacetate are linked to apoptosis induction brought on by elevated cytochrome c expression. T-cell differentiation is dependent on ROS and is induced by sodium dichloroacetate[1].
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| ln Vivo |
When male gonad-intact and castrated rats are treated with sodium dichloroacetate, the levels of NKCC1 RNA expression are markedly reduced; in contrast, no such effect is observed in female gonad-intact and castrated rats treated with sodium dichloroacetate[1]. In Wistar male rats, a single dose of sodium dichloroacetate results in a noticeably greater 24-hour diuresis; this increased diuresis is associated with NKCC2 inhibition. When comparing the kidneys of intact male and female Sprague-Dawley rats, the kidneys of intact female rats have more NKCC2 than the kidneys of intact male rats[1]. When male rats who are naïve are dosed 5, 20, and 100 mg/kg of sodium dichloroacetate orally, their bioavailability is significantly lower than that of rats whose GSTζ is depleted (10%, 13%, 81%, and 31%, 75%, 100%, respectively). Rats depleted of GSTζ exhibit linear kinetics for the liver extraction of sodium dichloroacetate; however, at higher doses, this process decreases with metabolism saturation[1].
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| Animal Protocol |
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| References |
[1]. Stakišaitis D, et al. The Importance of Gender-Related Anticancer Research on Mitochondrial Regulator Sodium Dichloroacetate in Preclinical Studies In Vivo. Cancers (Basel). 2019 Aug 20;11(8). pii: E1210.
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| Molecular Formula |
C2HCL2O2.NA
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| Molecular Weight |
150.92
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| CAS # |
2156-56-1
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| Related CAS # |
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| SMILES |
O=C([O-])C(Cl)Cl.[Na+]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (14.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (14.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (14.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (662.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.6260 mL | 33.1301 mL | 66.2603 mL | |
| 5 mM | 1.3252 mL | 6.6260 mL | 13.2521 mL | |
| 10 mM | 0.6626 mL | 3.3130 mL | 6.6260 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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