AK 295
Based on 1 Customer Validation
AK 295 (CX 295) is a selective calpain inhibitor. AK 295 can inhibit apoptosis through a calpain-dependent pathway. AK 295 shows potent neuroprotective effect. AK 295 can inhibit the activity of the cysteine protease calpain and reduce myocardial injury. AK 295 can be used for the researches of infection, inflammation, cardiovascular and neurological disease, such as stroke and viral myocarditis.
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- Purity: 99.0%
- CAS No.: 160399-35-9
- 화학식: C26H40N4O6
- 분자량:504.62
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
Calpain[1].
AK 295 (100 μM) inhibits the activity of the cysteine protease calpain in reovirus-infected primary cardiac myocytes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AK 295 (0.3-3 mg/kg, through the internal carotid artery, beginning 1.25 h from occlusion) protects against ischemic brain damage in stroke rats models[2].
AK 295 (70 mg/kg, i.p., once a day for 6 times) reduces reovirus myocarditis in reovirus strain 8B infection of neonatal mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats with spinal cord trauma[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneally injection, 1 hour after trauma
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Result:Reduced hemorrhage, edema, necrosis, and vascular thrombi.
Reduced apoptotic cell.
Improved motor dysfunction.
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Animal Model:Stroke rats models[2]
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Dosage:0.3, 0.75, 1.5 and 3 mg/kg
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Administration:Through the internal carotid artery, beginning 1.25 h from occlusion
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Result:Showed a 32% reduction in infarct volume 21 hours after the ischemia at 3 mg/kg.
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Animal Model:Reovirus strain 8B infection of neonatal mice[3]
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Dosage:70 mg/kg
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Administration:Intraperitoneally injection, once a day for 6 times
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Result:Inhibited apoptotic myocardial cell death.
Reduced serum creatine phosphokinase.
Improved weight gain.
Chemical Information
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CAS No. 160399-35-9
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Appearance Solid
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분자량 504.62
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화학식 C26H40N4O6
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Color White to off-white
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SMILES
O=C(N[C@@H](CC(C)C)C(NC(C(C(NCCCN1CCOCC1)=O)=O)CC)=O)OCC2=CC=CC=C2
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Synonyms
CX 295
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (198.17 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)
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 (4.95 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.95 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (273 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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Handling Instructions (2659 KB)
References
[1]. Colak A, et al. Calpain inhibitor AK 295 inhibits calpain-induced apoptosis and improves neurologic function after traumatic spinal cord injury in rats. Neurocirugia (Astur). 2009 Jun;20(3):245-54. [Content Brief]
[2]. Bartus RT, et al. Calpain inhibitor AK295 protects neurons from focal brain ischemia. Effects of postocclusion intra-arterial administration. Stroke. 1994 Nov;25(11):2265-70. [Content Brief]
[3]. DeBiasi RL, et al. Calpain inhibition protects against virus-induced apoptotic myocardial injury. J Virol. 2001 Jan;75(1):351-61. [Content Brief]
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 |
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| DMSO | 1 mM | 1.9817 mL | 9.9084 mL | 19.8169 mL | 49.5422 mL |
| 5 mM | 0.3963 mL | 1.9817 mL | 3.9634 mL | 9.9084 mL | |
| 10 mM | 0.1982 mL | 0.9908 mL | 1.9817 mL | 4.9542 mL | |
| 15 mM | 0.1321 mL | 0.6606 mL | 1.3211 mL | 3.3028 mL | |
| 20 mM | 0.0991 mL | 0.4954 mL | 0.9908 mL | 2.4771 mL | |
| 25 mM | 0.0793 mL | 0.3963 mL | 0.7927 mL | 1.9817 mL | |
| 30 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6514 mL | |
| 40 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2386 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9908 mL | |
| 60 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL | |
| 80 mM | 0.0248 mL | 0.1239 mL | 0.2477 mL | 0.6193 mL | |
| 100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4954 mL |
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