Ensitrelvir
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 500mg | $400 | Check With Us |
| 1g | $650 | Check With Us |
| 5g | $1645 | Check With Us |
: Cat #: V3351 CAS #: 2647530-73-0 Purity ≥ 99%
Description: Ensitrelvir (also known as S-217622; trade name Xocova) is an orally bioavailable, non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM) effective against the Omicron variant. On Nov 22, 2022, Ensitrelvir gained its first approval in Japan under the emergency regulatory approval system (EUA). It is an antiviral drug developed by Shionogi in partnership with Hokkaido University. It became the first Japanese domestic pill to treat COVID-19, third to be regulatorally approved in Japan; in February 2022.
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| Molecular Weight (MW) | 531.88 |
|---|---|
| Molecular Formula | C22H17ClF3N9O2 |
| CAS No. | 2647530-73-0 |
| SMILES Code | FC1=CC(CN(C(N2CC3=NN(C)C=N3)=O)/C(NC2=O)=N/C4=CC5=CN(C)N=C5C=C4Cl)=C(F)C=C1F |
| Synonyms | Ensitrelvir; Xocova; S217622; S-217622; S 217622; |
| Protocol | In Vitro | In a cytopathic effect (cpe)-inhibition assay of SARS-CoV-2 infected VeroE6/TMPRSS2 cells, Ensitrelvir shows the EC50 values are approximately 0.4 μM for both wild-type virus and Alpha, Beta, Gamma and Delta variants. EC50 values for SARS-CoV and MERS-CoV were 0.21 and 1.4 μM respectively[1]. The antiviral activities were evaluated as per their inhibitory ability of the cytopathic effects elicited in SARS-CoV-2-infected VeroE6/TMPRSS2 cells. S-217622 exhibited similar antiviral activities against all tested SARS-CoV-2 variants, including the Omicron strain, which is responsible for the current wave of the pandemic, indicating its potential broad usability as a therapeutic agent for treating COVID-19 (half-maximal effective concentration [EC50] = 0.29–0.50 μM. Antiviral activity of S-217622 against SARS-CoV (EC50 = 0.21 μM). was also comparable to that against SARS-CoV-2, where the sequence homology of 3CLpro between SARS-CoV-2 and SARS-CoV was well-conserved. S-217622 also exhibited potent antiviral activity against MERS-CoV (EC50 = 1.4 μM), HCoV-OC43 (EC90 = 0.074 μM), and HCoV-229E (EC50 = 5.5 μM). S-217622 showed no inhibitory activity against host-cell proteases, such as caspase-2, chymotrypsin, cathepsin B/D/G/L, and thrombin at up to 100 μM, suggesting its high selectivity for coronavirus proteases. S-217622 exhibited no safety concerns in vitro in studies involving ether-a-go-go-related gene inhibition, mutagenicity/clastogenicity, and phototoxicity. [3] |
|---|---|---|
| In Vivo | Ensitrelvir dose-dependently inhibits intrapulmonary replication of SARS-CoV-2 in mice[2]. The antiviral efficacy of S-217622 was evaluated in vivo in mice infected with SARS-CoV-2 Gamma strain. Five-week-old BALB/c mice were intranasally inoculated with SARS-CoV-2 Gamma strain (hCoV-19/Japan/TY7-501/2021), and S-217622 was administered orally as a 0.5% methylcellulose suspension immediately and 12 hours after infection. S-217622 treatment reduced the intrapulmonary viral titers dose-dependently. The mean viral titer was significantly lower in the S-217622 treatment groups than in the vehicle treatment group (2 mg/kg vs vehicle, p = 0.0289; 8, 16, and 32 mg/kg vs vehicle, p < 0.0001). Viral titers reached near the lower limit of quantification (1.80 – log10 50% tissue culture infectious dose [TCID50]/mL) at 16 and 32 mg/kg in the S-217622 treatment group. Although twice-daily treatment was applied in this mouse model, a once-daily treatment model could be applicable in clinical treatment because S-217622 showed a much lower clearance and longer elimination half-lives in nonrodents than in rodents. [3] |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8801 mL | 9.4006 mL | 18.8012 mL | 37.6025 mL |
| 5mM | 0.3760 mL | 1.8801 mL | 3.7602 mL | 7.5205 mL |
| 10mM | 0.1880 mL | 0.9401 mL | 1.8801 mL | 3.7602 mL |
| 20mM | 0.0940 mL | 0.4700 mL | 0.9401 mL | 1.8801 mL |
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