CAST-calpain-2 stabilizer-1
Based on 1 Customer Validation
CAST-calpain-2 stabilizer-1 is a blood-brain barrier permeable stabilizer of CAST-calpain-2 interaction. CAST-calpain-2 stabilizer-1 shows no activity against GSK3. CAST-calpain-2 stabilizer-1 can be used in the research of Huntington's disease and tauopathies.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.80%
- CAS No.: 3110929-05-7
- Formule: C22H20Cl2N6O2
- Masse moléculaire:471.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
CAST-calpain-2 stabilizer-1 (dose-response range) potently restores mitochondrial membrane potential in HdhQ111 mouse striatal neuron-like cells with an EC50 of ~2.77 μM[1].
CAST-calpain-2 stabilizer-1 (0-20 μM) upregulates CAST protein expression in HdhQ111 mouse striatal neuron-like cells with an EC50 of ~3.55 μM[1].
CAST-calpain-2 stabilizer-1 (0.625-10 μM) reduces mitochondrial ROS production in HdhQ111 mouse striatal neuron-like cells with an IC50 of ~1.43 μM[1].
CAST-calpain-2 stabilizer-1 enhances the endogenous interaction between CAST and calpain-2 in HdhQ111 mouse striatal neuron-like cells[1].
CAST-calpain-2 stabilizer-1 (0-500 μM; 40 min (with lysates); 5 min (Pronase digestion)) directly binds and stabilizes CAST protein in HdhQ111 mouse striatal neuron-like cell lysates in a dose-dependent manner[1].
CAST-calpain-2 stabilizer-1 (10 μM (TMRM assay); 5-10 μM (MTT assay); 48 h (TMRM assay)) requires endogenous CAST and calpain-2 to exert its mitochondrial protective and viability-enhancing effects in HdhQ111 mouse striatal neuron-like cells[1].
CAST-calpain-2 stabilizer-1 (1 μM; 5 consecutive days) restores neuronal marker expression, suppresses calpain-2 activity, and rescues neurite outgrowth in human patient iPSC-derived HD medium spiny neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:HdhQ111 mouse striatal neuron-like cells
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Concentration:5-10 μM
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Incubation Time:5-10 μM (MTT assay); 48 h (TMRM assay)
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Result:Exerted mitochondrial protective and viability-enhancing effects in HdhQ111 mouse striatal neuron-like cell with endogenous CAST and calpain-2.
In Vivo
CAST-calpain-2 stabilizer-1 (10 mg/kg; i.p.; 5 days per week; 5 months) restores CAST-calpain-2 signaling, reduces tauopathy-associated neuropathology and neuroinflammation, and improves both short-term and long-term memory in PS19 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6;C3Tg (Prnp-MAPT*P301S) PS19 (male, tauopathy model expressing mutant P301S human tau protein)[1]
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Dosage:10 mg/kg
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Administration:i.p.; once daily, 5 days per week; 5 months
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Result:Improved short-term memory, as shown by enhanced spontaneous alternation performance in the Y maze test.
Improved long-term memory, as shown by reduced escape latency in the Barnes maze test.
Reduced hippocampal phosphorylated tau (AT8-positive) levels.
Reduced neuroinflammation, as shown by decreased IBA1 (microglia) and GFAP (astrocyte) immunodensity in the hippocampus.
Restored hippocampal CAST protein expression and reduced cleavage of calpain-2 substrates (α-spectrin, p35 to p25).
Reduced hippocampal Drp1 phosphorylation at Ser616.
Restored the interaction between endogenous CAST and calpain-2 in hippocampal tissue.
Chemical Information
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CAS No. 3110929-05-7
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Appearance Solid
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Masse moléculaire 471.34
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Formule C22H20Cl2N6O2
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Color Light yellow to green yellow
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SMILES
N#CC1=CN=C(C=C1)OCCNC2=NC=C(N3CCOCC3)C(C4=C(Cl)C=C(Cl)C=C4)=N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (212.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1216 mL | 10.6081 mL | 21.2161 mL | 53.0403 mL |
| 5 mM | 0.4243 mL | 2.1216 mL | 4.2432 mL | 10.6081 mL | |
| 10 mM | 0.2122 mL | 1.0608 mL | 2.1216 mL | 5.3040 mL | |
| 15 mM | 0.1414 mL | 0.7072 mL | 1.4144 mL | 3.5360 mL | |
| 20 mM | 0.1061 mL | 0.5304 mL | 1.0608 mL | 2.6520 mL | |
| 25 mM | 0.0849 mL | 0.4243 mL | 0.8486 mL | 2.1216 mL | |
| 30 mM | 0.0707 mL | 0.3536 mL | 0.7072 mL | 1.7680 mL | |
| 40 mM | 0.0530 mL | 0.2652 mL | 0.5304 mL | 1.3260 mL | |
| 50 mM | 0.0424 mL | 0.2122 mL | 0.4243 mL | 1.0608 mL | |
| 60 mM | 0.0354 mL | 0.1768 mL | 0.3536 mL | 0.8840 mL | |
| 80 mM | 0.0265 mL | 0.1326 mL | 0.2652 mL | 0.6630 mL | |
| 100 mM | 0.0212 mL | 0.1061 mL | 0.2122 mL | 0.5304 mL |
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