| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
Caspases-3 is inhibited by cystamine, with an IC50 value of 23.6 μM[1]. Recombinant active caspase-3 is inhibited by cystamine (0-500 μM; 0-16 hours) in a concentration-dependent manner [1]. Glutathione levels are markedly elevated by cystamine (250 μM; 10 hours) [1].
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|---|---|
| ln Vivo |
R6/2 transgenic HD mice that receive cystamine (oral, i.p.; 112, 225 mg/kg) have reduced behavioral and neuropathological severity, decreased Tgase activity, and extended longevity [2].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Human Neuroblastoma SH-SY5Y Cell Tested Concentrations: 250, 500 μM Incubation Duration: 0-16 h Experimental Results: Inhibition of MG132-mediated caspase-3 activation. Inhibits H2O2-mediated caspase-3 activation. Inhibits caspase-3 activity in a tTG-independent manner. |
| Animal Protocol |
Animal/Disease Models: R6/2 transgenic HD mice [2]
Doses: 112, 225 mg/kg Route of Administration: intraperitonealor po (po (oral gavage)) daily Experimental Results: Dramatically prolonged survival, improved body weight and exercise capacity, and delayed neuropathological sequelae And Dramatically altered neuropathological sequelae were the levels of Tgase activity and N(Sigma)-(gamma-L-glutamyl)-L-lysine (GGEL) levels. |
| References |
[1]. Mathieu Lesort, et al. Cystamine inhibits caspase activity. Implications for the treatment of polyglutamine disorders. J Biol Chem. 2003 Feb 7;278(6):3825-30.
[2]. Alpaslan Dedeoglu, et al. Therapeutic effects of cystamine in a murine model of Huntington's disease. J Neurosci. 2002 Oct 15;22(20):8942-50. [3]. Thomas M Jeitner, et al. Cystamine and cysteamine as inhibitors of transglutaminase activity in vivo. Biosci Rep. 2018 Sep 5;38(5):BSR20180691. |
| Molecular Formula |
C4H12N2S2
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|---|---|
| Molecular Weight |
152.27
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| Exact Mass |
152.0442
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| CAS # |
51-85-4
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| Related CAS # |
Cystamine (dihydrochloride）;56-17-7
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C(N)CSSCCN
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| Synonyms |
Mercamine disulfide; Aminoethyl-SS-ethylamine; Cystamine
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~656.69 mM)
H2O : ~100 mg/mL (~656.69 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (16.42 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 25.0 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: ≥ 2.5 mg/mL (16.42 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 25.0 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: ≥ 2.5 mg/mL (16.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.5673 mL | 32.8364 mL | 65.6728 mL | |
| 5 mM | 1.3135 mL | 6.5673 mL | 13.1346 mL | |
| 10 mM | 0.6567 mL | 3.2836 mL | 6.5673 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02304666 | Unknown | Procedure: Colonoscopy for biopsies samples |
Inflammatory Bowel Disease | Assistance Publique Hopitaux De Marseille |
November 2014 | Not Applicable |
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