Leritrelvir

SKU: orb1744472

Description

Leritrelvir (RAY1216) is a potent, orally bioavailable SARS-CoV-2 main protease (Mpro) inhibitor. It functions by blocking the cleavage of viral polyproteins, thereby suppressing viral replication. This small molecule is a valuable research tool for in vitro antiviral assays and in vivo studies exploring therapeutic interventions against COVID-19.

Research Area

Infectious Disease & Virology

Key Properties

• CAS Number: 2923310-64-7
• MW: 639.71
• Purity: 97.42%
• Formula: C₃₁H₄₄F₃N₅O₆
• SMILES: C(N[C@@H](C[C@H]1C(=O)NCC1)C(C(NC2CCCC2)=O)=O)(=O)[C@H]3N(C([C@@H](NC(C(F)(F)F)=O)[C@H]4CCCCC4)=O)C[C@]5([C@@]3(CCC5)[H])[H]
• Target: SARS-CoV

Bioactivity

• In Vivo:
  Leritrelvir was effective in prolonging the survival time of SARS-CoV-2 infected mice for 5 consecutive days under oral administration conditions in the dose range of 150-600 mg/kg/day. The pharmacokinetic parameters of the drug have been studied in a variety of animals demonstrating the exposure and metabolic properties of the drug. In mice, the area under the drug curve (AUC(0-last)) at an intravenous (IV) dose of 3.0 mg/kg was 7789 nM/h, but peak concentration (C_max) and time to peak (T_max) were not provided. In comparison, an oral (PO) dose of 10 mg/kg produced a C_max of 1287 nM, a T_max of 2.0 hours, an AUC(0-last) of 5698 nM/h, an elimination half-life (T_1/2) of 2.6 hours, and an oral bioavailability (F%) of 22. In rats, the intravenous (IV) dose of 2.0 mg/kg yielded an AUC(0-last) of 4505 nM/h, whereas the oral (PO) dose of 10 mg/kg produced a C_max of 916 nM, a T_max of 0.9 h, an AUC(0-last) of 7429 nM/h, a T_1/2 of 4.3 h, and an F% of 33. In cynomolgus monkeys, the intravenous (IV) dose of 1.0 mg/kg had an AUC(0-last) of 1157 nM/h, whereas the oral (PO) dose of 5.0 mg/kg yielded a C_max of 102 nM, a T_max of 1.5 h, an AUC(0-last) of 458 nM/h, a T_1/2 of 14.9 h, and a F% of 8.
• In Vitro:
  Leritrelvir has a residence time of 104 minutes on the target. Leritrelvir forms covalent binding to the Cys145 catalytic site via the α-ketoamide warhead. 0-1000 nM Leritrelvir, treated for 72 hours, demonstrated antiviral effects against SARS-CoV-2 wild type and its variants.

Storage & Handling

• Storage: keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SARSCoV, SARS-CoV-2, RAY 1216, RAY1216

Compound Identifiers

PubChem CID

167713195