2. Anti-infection
  3. SARS-CoV
  4. Leritrelvir

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

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Leritrelvir Chemical Structure

Leritrelvir Chemical Structure

CAS No. : 2923310-64-7

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Leritrelvir Related Antibodies

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Description

Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a Ki of 8.6 nM[1].

IC50 & Target

Ki: 8.6 nM (SARS-CoV-2 main protease)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Leritrelvir Related Antibodies

Cell Viability Assay[1]

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.
In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female human ACE2 transgenic C57BL/6 mouse, SARS-CoV-2 infection model[1]
Dosage: 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[1]
Dosage: 1-10 mg/kg
Administration: PO or IV (Pharmacokinetic Analysis)
Result: Showed promising human pharmacokinetics profile.
Clinical Trial
Molecular Weight

639.71

Formula

C31H44F3N5O6
CAS No.
SMILES

O=C(C(F)(F)F)N[C@H](C(N1C[C@H](CCC2)[C@H]2[C@H]1C(N[C@@H](C[C@]3([H])CCNC3=O)C(C(NC4CCCC4)=O)=O)=O)=O)C5CCCCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Leritrelvir Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Leritrelvir2923310-64-7RAY1216RAY 1216RAY-1216SARS-CoVSARS coronavirusantiviralSARS-CoV-2OmicronC57BL/6Vero E6Inhibitorinhibitorinhibit

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