| Field | Specification |
|---|---|
| Alternative names | U 74006F free base |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C38H52N6O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Tirilazad, also known as U 74006F free base, is a neuroprotective agent that can also bind tightly to the main protease of the COVID-19 virus and exert anti-SARS-CoV-2 activity. It scavenges hydroxyl and lipid peroxyl free radicals, helps maintain levels of endogenous antioxidants, and in animal models of focal ischemia reduces cerebral infarct volume while improving neurobehavioral scores. The compound can be used in research on ischemic stroke and subarachnoid hemorrhage[1]. It is supplied as an off-white to light yellow solid (C38H52N6O2, MW 624.86) at 97.03% purity.
Physical & Chemical Properties
| CAS Number | 110101-66-1 |
|---|---|
| Molecular Formula | C38H52N6O2 |
| Molecular Weight | 624.86 g/mol |
| Purity | 97.03% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | C[C@@]12[C@](C[C@H]([C@@H]2C(CN3CCN(C4=NC(N5CCCC5)=NC(N6CCCC6)=C4)CC3)=O)C)([H])[C@@]7([H])C([C@@]8(C(CC7)=CC(C=C8)=O)C)=CC1 |
| Signaling Pathway | Immunology/Inflammation; NF-κB; Metabolic Enzyme/Protease; Anti-infection |
| Solubility | In Vitro: DMSO: 33.33 mg/mL (53.34 mM; Requires sonication and warming and heat to 60°C; 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 | 33.33 mg/mL (53.34 mM) | requires sonication and warming and heat to 60°C; 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 | ≥ 3.33 mg/mL (5.33 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.33 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (33.3 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% Corn Oil |
|---|---|
| Result | ≥ 3.33 mg/mL (5.33 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.33 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 (33.3 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vivo
In rat and rabbit models of focal cerebral ischemia, Tirilazad (single administration, i.v./i.p., 0-40 mg/kg; within 6 h from pre- to post-ischemia) significantly decreases infarct volume and improves neurobehavioral scores[1].
| Animal Model | Rats, Rabbits, Cats[1] |
|---|---|
| Dosage | 0-40 mg/kg |
| Administration | i.v./i.p.; single administration; within 6 h from pre- to post-ischemia |
| Result | Reduced infarct volume by 29.2% and improved neurobehavioral score by 48.1% in animal models of focal cerebral ischemia, with optimal efficacy at 3-9.9 mg/kg, higher efficacy in temporary occlusion models than in permanent or thrombotic models, and no efficacy in feline models. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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