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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Salpyran dihydrochloride targets copper(II) ions in biological systems, not a traditional protein receptor or enzyme. It acts as a tetradentate ligand that coordinates specifically with Cu2+ to form a stable complex. By binding to and sequestering Cu2+, it prevents the metal ion from participating in redox reactions that generate reactive oxygen species (ROS), thereby mitigating oxidative stress.
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| ln Vitro |
In vitro, Salpyran dihydrochloride effectively prevents the formation of reactive oxygen species (ROS) in the binary Cu(II)/H2O2 system. The compound functions as a potent Cu(II) scavenger, reducing oxidative damage in test systems. It can also be used to study the role of copper in biological processes, as its high selectivity allows it to disrupt cellular copper homeostasis without affecting other essential metal ions.
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| ln Vivo |
In vivo activity data for Salpyran dihydrochloride have not been detailed in the provided references. Based on its mechanism as a Cu(II) selective chelator, it is hypothesized to be protective in animal models of diseases where copper toxicity is implicated, such as Wilson's disease, certain cancers, and neurodegenerative disorders. Its potential to reduce oxidative stress suggests it could have therapeutic potential, but this requires further in vivo validation.
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| Enzyme Assay |
The ability of Salpyran dihydrochloride to bind copper(II) can be evaluated using a cell-free spectrophotometric titration. A fixed concentration of CuSO4 (e.g., 20 microM) is added to a solution containing increasing concentrations of Salpyran (0-100 microM) in a buffer (e.g., HEPES, pH 7.4). The formation of the Cu(II)-Salpyran complex can be monitored by measuring the change in absorbance at a specific wavelength (e.g., 550 nm) on a UV-Vis spectrophotometer. The binding constant (Ka) can be calculated from the titration data to determine the chelator's affinity for Cu(II).
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| Cell Assay |
Salpyran dihydrochloride can be used to study copper-dependent processes in cell culture models. Cells are seeded in 6- or 96-well plates and allowed to adhere overnight. They are then exposed to Salpyran (1-50 microM) for 24-48 h. The compound's effect on cellular copper levels can be assessed using inductively coupled plasma mass spectrometry (ICP-MS). Its ability to mitigate oxidative stress can be measured by quantifying intracellular reactive oxygen species (ROS) using the fluorescent dye DCFH-DA. Cytotoxicity is assessed by the MTT assay to determine non-toxic concentration ranges.
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| Animal Protocol |
Salpyran dihydrochloride can be studied in animal models of copper overload, such as the Long-Evans Cinnamon (LEC) rat model of Wilson's disease. LEC rats, which accumulate copper in the liver, are treated daily with Salpyran (2.5-10 mg/kg, i.p.) for 4-8 weeks. The effect on copper levels is measured by ICP-MS in liver and brain tissue. Markers of oxidative stress (e.g., malondialdehyde, glutathione) are measured in tissue homogenates. Hepatic and neurological function is assessed via blood biochemistry and behavioral tests.
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| ADME/Pharmacokinetics |
Salpyran dihydrochloride has a molecular weight of 330.25 and a molecular formula of C15H21Cl2N3O. It is stored at 4degC in a sealed container away from moisture. For solubility, it is soluble in DMSO at 100 mg/mL (302.80 mM). The product should be stored as a powder at 4degC for up to 2 years, and in solvent at -80degC for 6 months or -20degC for 1 month. Specific pharmacokinetic parameters are not available.
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| Toxicity/Toxicokinetics |
As a selective copper(II) chelator, the primary safety concern of Salpyran is the potential for disrupting essential copper-dependent enzymes, leading to copper deficiency if used at high doses chronically. However, no detailed toxicity data are available. In vitro studies indicate it is well-tolerated at low micromolar concentrations. Standard safety precautions for handling chelators and potential metal toxicants should be followed, including the use of PPE to avoid inhalation or skin contact.
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| References |
[1]. Devonport J, et al. Salpyran: A Cu(II) Selective Chelator with Therapeutic Potential. Inorg Chem. 2021 Oct 18;60(20):15310-15320.
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| Additional Infomation |
Salpyran dihydrochloride is a research-grade compound and is not approved for clinical use. It is a novel tetradentate ligand with high selectivity for copper(II) ions, designed for research into copper-related diseases and oxidative stress. It is derived from the salpyran scaffold and has been studied for its potential to prevent ROS formation. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C15H21CL2N3O
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| Related CAS # |
Salpyran;2719737-44-5;Salpyran hydrochloride
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| Appearance |
Light yellow to brown solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
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
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| 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.) |
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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