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[CAS NO. 2647530-73-0] Ensitrelvir
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-143216 |
| Brand: | MCE |
| CAS: | 2647530-73-0 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 531.88 |
| Molecular Formula | C22H17ClF3N9O2 |
| SMILES | FC1=C(CN2C(N(CC3=NN(C)C=N3)C(N/C2=N\C4=CC5=CN(C)N=C5C=C4Cl)=O)=O)C=C(F)C(F)=C1 |
Summary
In Vitro
In a cytopathic effect (cpe)-inhibition assay of SARS-CoV-2 infected VeroE6/TMPRSS2 cells, Ensitrelvir shows the EC 50 values are approximately 0.4 μM for both wild-type virus and Alpha, Beta, Gamma and Delta variants. EC 50 values for SARS-CoV and MERS-CoV were 0.21 and 1.4 μM respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ensitrelvir dose-dependently inhibits intrapulmonary replication of SARS-CoV-2 in mice [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT05409911 | Shionogi|Shionogi Inc. |
Hepatic Impairment
|
September 13, 2022 | Phase 1 |
| NCT05305547 | Shionogi|National Institute of Allergy and Infectious Diseases (NIAID)|Shionogi Inc. |
SARS-CoV-2 Infection
|
August 3, 2022 | Phase 3 |
| NCT05363215 | Shionogi|Shionogi Inc. |
Renal Impairment
|
August 10, 2022 | Phase 1 |
| NCT05605093 | University of Minnesota|National Institute of Allergy and Infectious Diseases (NIAID) |
COVID-19
|
November 1, 2022 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 94.01 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8801 mL | 9.4006 mL | 18.8012 mL |
| 5 mM | 0.3760 mL | 1.8801 mL | 3.7602 mL |
| 10 mM | 0.1880 mL | 0.9401 mL | 1.8801 mL |
References
- [1] McKimm-Breschkin JL, et al. COVID-19, Influenza and RSV: Surveillance-informed prevention and treatment - Meeting report from an isirv-WHO virtual conference. Antiviral Res. 2022;197:105227.
- [2] Yuto Unoh, et al. Discovery of S-217622, a Non-Covalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19. bioRxiv 2022.01.26.477782.
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