Leritrelvir

Research use only, not for human use.

Leritrelvir (RAY1216) is a potent orally active inhibitor of the SARS-CoV-2 main protease, exhibiting a slow-tight binding mechanism with an inhibition constant (Ki) of 8.6 nM .

Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a Ki of 8.6 nM.

Cell Viability Assay Cell Line:Vero E6 cells inoculated with SARS-CoV-2 WT, Alpha, Beta, Delta, Omicron BA.1 and Omicron 247 BA.5 strains Concentration:0-1000 nM Incubation Time:72 h Result:The half-maximal effective concentration (EC50) values against different SARS-CoV-2 variants were 95 nM (WT), 130 nM (Alpha), 277 nM (Beta), 97 nM (Delta), 86 nM (Omicron BA.1) and 158 nM (Omicron BA.5), respectively.

Oral bioavailabilityAnimal Model:Female human ACE2 transgenic C57BL/6 mouse, SARS-CoV-2 infection modelDosage:150, 300 and 600 mg/kg/day Administration:Intragastric administration, 5 days Result:Protected mice infected with SARS-CoV-2 by 100%, 43% and 14% at 600, 300 and 150 mg/kg, respectively. Decreased viral titres in lungs significantly compared with the infection-only group. Reduced virus induced pathology. Animal Model:Male CD-1 mouse, male SD rat and male cynomolgus macaque Dosage:1-10 mg/kg Administration:PO or IV (Pharmacokinetic Analysis)Result:Showed promising human pharmacokinetics profile.

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Others

Other Targets

SARS-CoV

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2923310-64-7

639.71

C31H44F3N5O6

>98% (HPLC)

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C1CCC(CC1)[C@@H](C(=O)N2C[C@@H]3CCC[C@@H]3[C@H]2C(=O)N[C@@H](C[C@@H]4CCNC4=O)C(=O)C(=O)NC5CCCC5)NC(=O)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years