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编 号：F756917
分子式：C31H44F3N5O6
分子量：639.71
分子式：C31H44F3N5O6
分子量：639.71
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CAS No: 2923310-64-7
产品详情
生物活性：
Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a Ki of 8.6 nM.
体内研究：
Leritrelvir (RAY1216) (150-600 mg/kg/day; i.g.; 5 days) 有效延长 SARS-CoV-2 感染小鼠的生存。Compound pharmacokinetics parameters in different animal speciesCompoundSpecies dose (mg/kg) Cmax (nM) Tmax (h) AUC(0-last) (nM?h) Cl (mL/min/kg) Vdss (L/kg) T1/2 (h) oral F (%)
Mouse3.0 (IV)--7789101.43.8-
10 (PO)12872.05698--2.622
Leritrelvirrat2.0 (IV)--450512.51.12.2-
10 (PO)9160.97429--4.333
cynomolgus macaque1.0 (IV)--115722.51.00.9-
5.0 (PO)1021.5458--14.98
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 CmaxAUC: “Area Under the Curve” and represents the total exposure of the drug experienced by the subject in a clinical studyCl: total plasma clearanceVdss: Steady state volume of distributionT1/2: Half-time is the time it takes for half the drug concentration to be eliminatedoral (F%): Oral bioavailabilityAnimal Model:Female human ACE2 transgenic C57BL/6 mouse, SARS-CoV-2 infection model
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
Dosage:1-10 mg/kg
Administration:PO or IV (Pharmacokinetic Analysis)
Result:Showed promising human pharmacokinetics profile.
体外研究：
Leritrelvir (RAY1216) 的药物靶向停留时间为 104 分钟。Leritrelvir 通过 α-ketoamide warhead 共价连接到催化的 Cys145 上。Leritrelvir (0-1000 nM; 72 h) 显示出对 SARS-CoV-2 野生型祖先株和变异株的抗病毒活性。
Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a Ki of 8.6 nM.
体内研究：
Leritrelvir (RAY1216) (150-600 mg/kg/day; i.g.; 5 days) 有效延长 SARS-CoV-2 感染小鼠的生存。Compound pharmacokinetics parameters in different animal speciesCompoundSpecies dose (mg/kg) Cmax (nM) Tmax (h) AUC(0-last) (nM?h) Cl (mL/min/kg) Vdss (L/kg) T1/2 (h) oral F (%)
Mouse3.0 (IV)--7789101.43.8-
10 (PO)12872.05698--2.622
Leritrelvirrat2.0 (IV)--450512.51.12.2-
10 (PO)9160.97429--4.333
cynomolgus macaque1.0 (IV)--115722.51.00.9-
5.0 (PO)1021.5458--14.98
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 CmaxAUC: “Area Under the Curve” and represents the total exposure of the drug experienced by the subject in a clinical studyCl: total plasma clearanceVdss: Steady state volume of distributionT1/2: Half-time is the time it takes for half the drug concentration to be eliminatedoral (F%): Oral bioavailabilityAnimal Model:Female human ACE2 transgenic C57BL/6 mouse, SARS-CoV-2 infection model
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
Dosage:1-10 mg/kg
Administration:PO or IV (Pharmacokinetic Analysis)
Result:Showed promising human pharmacokinetics profile.
体外研究：
Leritrelvir (RAY1216) 的药物靶向停留时间为 104 分钟。Leritrelvir 通过 α-ketoamide warhead 共价连接到催化的 Cys145 上。Leritrelvir (0-1000 nM; 72 h) 显示出对 SARS-CoV-2 野生型祖先株和变异株的抗病毒活性。
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