Tirilazad
Based on 1 Customer Validation
Tirilazad (U 74006F free base) is a neuroprotective agent. Tirilazad can also bind tightly to the main protease of the COVID-19 virus and exert anti-SARS-CoV-2 activity. Tirilazad scavenges hydroxyl and lipid peroxyl free radicals and maintains the levels of endogenous antioxidants. Tirilazad reduces cerebral infarct volume and improves neurobehavioral scores in animal models of focal ischemia. Tirilazad can be used in research related to ischemic stroke and subarachnoid hemorrhage.
For research use only. We do not sell to patients.
- Purity: 98.11%
- CAS No.: 110101-66-1
- Formula: C38H52N6O2
- Molecular Weight:624.86
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats, Rabbits, Cats[1]
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Dosage:0-40 mg/kg
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Administration:i.v./i.p.; single administration; within 6 h from pre- to post-ischemia
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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.
Chemical Information
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CAS No. 110101-66-1
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Appearance Solid
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Molecular Weight 624.86
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Formula C38H52N6O2
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Color Off-white to light yellow
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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
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Synonyms
U 74006F free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 33.33 mg/mL (53.34 mM; ultrasonic and warming and heat to 60°C; 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: ≥ 3.33 mg/mL (5.33 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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.
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.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Sena E, et al. Systematic review and meta-analysis of the efficacy of tirilazad in experimental stroke. Stroke. 2007;38(2):388-394. [Content Brief]
[2]. Chtita S, et al. Discovery of Potent SARS-CoV-2 Inhibitors from Approved Antiviral Drugs via Docking and Virtual Screening. Comb Chem High Throughput Screen. 2021;24(3):441-454. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6004 mL | 8.0018 mL | 16.0036 mL | 40.0090 mL |
| 5 mM | 0.3201 mL | 1.6004 mL | 3.2007 mL | 8.0018 mL | |
| 10 mM | 0.1600 mL | 0.8002 mL | 1.6004 mL | 4.0009 mL | |
| 15 mM | 0.1067 mL | 0.5335 mL | 1.0669 mL | 2.6673 mL | |
| 20 mM | 0.0800 mL | 0.4001 mL | 0.8002 mL | 2.0004 mL | |
| 25 mM | 0.0640 mL | 0.3201 mL | 0.6401 mL | 1.6004 mL | |
| 30 mM | 0.0533 mL | 0.2667 mL | 0.5335 mL | 1.3336 mL | |
| 40 mM | 0.0400 mL | 0.2000 mL | 0.4001 mL | 1.0002 mL | |
| 50 mM | 0.0320 mL | 0.1600 mL | 0.3201 mL | 0.8002 mL |