Leritrelvir |
Catalog No.GC71221
One-Click Copy Product Info
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Leritrelvir (RAY1216) es un inhibiinhibidor lento de la proteasa SARS-CoV-2 con un Ki de 8,6 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2923310-64-7
Sample solution is provided at 25 µL, 10mM.
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Leritrelvir (RAY1216) has a drug-target residence time of 104 min[1].
Leritrelvir is covalently attached to the catalytic Cys145 through the α-ketoamide warhead[1].
Leritrelvir (0-1000 nM; 72 h) shows antiviral activities against SARS-CoV-2 wild type ancestral strain and variants[1].
Leritrelvir (RAY1216 (150-600 mg/kg/day; i.g.; 5 days) effectively prolongs survival of SARS-CoV-2 infected mice[1].
Compound pharmacokinetics parameters in different animal species[1]
| Compound | Species | dose (mg/kg) | Cmax (nM) | Tmax (h) | AUC(0-last) (nM•h) | Cl (mL/min/kg) | Vdss (L/kg) | T1/2 (h) | oral F (%) |
| Mouse | 3.0 (IV) | - | - | 7789 | 10 | 1.4 | 3.8 | - | |
| 10 (PO) | 1287 | 2.0 | 5698 | - | - | 2.6 | 22 | ||
| RAY1216 | rat | 2.0 (IV) | - | - | 4505 | 12.5 | 1.1 | 2.2 | - |
| 10 (PO) | 916 | 0.9 | 7429 | - | - | 4.3 | 33 | ||
| cynomolgus macaque | 1.0 (IV) | - | - | 1157 | 22.5 | 1.0 | 0.9 | - | |
| 5.0 (PO) | 102 | 1.5 | 458 | - | - | 14.9 | 8 |
Cmax: the maximum observed concentration of the drug collected in bodily material from subjects in a clinical study
Tmax: the time it takes to reach the maximum concentration or time to Cmax
AUC: “Area Under the Curve” and represents the total exposure of the drug experienced by the subject in a clinical study
Cl: total plasma clearance
Vdss: Steady state volume of distribution
T1/2: Half-time is the time it takes for half the drug concentration to be eliminated
oral (F%): Oral bioavailability
References:
[1]. Chen X, et al. Inhibition mechanism and antiviral activity of an α-ketoamide based SARS-CoV-2 main protease inhibitor. bioRxiv, 2023: 2023.03. 09.531862.
| Cas No. | 2923310-64-7 | SDF | |
| Formula | C31H44F3N5O6 | M.Wt | 639.71 |
| Solubility | Storage | -20°C, protect from light | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5632 mL | 7.816 mL | 15.6321 mL |
| 5 mM | 312.6 μL | 1.5632 mL | 3.1264 mL |
| 10 mM | 156.3 μL | 781.6 μL | 1.5632 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)