| Field | Specification |
|---|---|
| Alternative names | CX 295 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H40N4O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
AK 295, also known as CX 295, is a selective calpain inhibitor that can inhibit apoptosis through a calpain-dependent pathway and shows a potent neuroprotective effect. It can inhibit the cysteine protease calpain and reduce myocardial injury, and it can be used in research on infection, inflammation, and cardiovascular and neurological diseases such as stroke and viral myocarditis[1][2][3]. It is supplied as a white to off-white solid (C26H40N4O6, MW 504.62) at 99.0% purity.
Physical & Chemical Properties
| CAS Number | 160399-35-9 |
|---|---|
| Molecular Formula | C26H40N4O6 |
| Molecular Weight | 504.62 g/mol |
| Purity | 99.0% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(N[C@@H](CC(C)C)C(NC(C(C(NCCCN1CCOCC1)=O)=O)CC)=O)OCC2=CC=CC=C2 |
| Signaling Pathway | Metabolic Enzyme/Protease; Apoptosis |
| Solubility | In Vitro: DMSO: 100 mg/mL (198.17 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (198.17 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (4.95 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (4.95 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (4.95 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In reovirus-infected primary cardiac myocytes, AK 295 (100 μM) inhibits the activity of the cysteine protease calpain[3].
In Vivo
In rats with spinal cord trauma, apoptosis is inhibited and neurologic function improved by AK 295 (2 mg/kg, i.p., 1 hour after trauma)[1]. In stroke rat models, AK 295 (0.3-3 mg/kg, delivered through the internal carotid artery, starting 1.25 h from occlusion) protects against ischemic brain damage[2]. Reovirus myocarditis is reduced by AK 295 (70 mg/kg, i.p., once a day for 6 times) in neonatal mice infected with reovirus strain 8B[3].
| Animal Model | Rats with spinal cord trauma[1] |
|---|---|
| Dosage | 2 mg/kg |
| Administration | Intraperitoneally injection, 1 hour after trauma |
| Result | Reduced hemorrhage, edema, necrosis, and vascular thrombi. Reduced apoptotic cell. Improved motor dysfunction. |
| Animal Model | Stroke rats models[2] |
|---|---|
| Dosage | 0.3, 0.75, 1.5 and 3 mg/kg |
| Administration | Through the internal carotid artery, beginning 1.25 h from occlusion |
| Result | Showed a 32% reduction in infarct volume 21 hours after the ischemia at 3 mg/kg. |
| Animal Model | Reovirus strain 8B infection of neonatal mice[3] |
|---|---|
| Dosage | 70 mg/kg |
| Administration | Intraperitoneally injection, once a day for 6 times |
| Result | Inhibited apoptotic myocardial cell death. Reduced serum creatine phosphokinase. Improved weight gain. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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