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Leritrelvir

CAS No. :

產品活性：Leritrelvir (RAY1216) is an orally active SARS-CoV-2 main protease slow-tight inhibitor with a K_i of 8.6 nM.

研究領域：Anti-infection

作用靶點：SARS-CoV

In Vitro: Leritrelvir (RAY1216) has a drug-target residence time of 104 min.
Leritrelvir is covalently attached to the catalytic Cys145 through the α-ketoamide warhead.
Leritrelvir (0-1000 nM; 72 h) shows antiviral activities against SARS-CoV-2 wild type ancestral strain and variants.

In Vivo: Leritrelvir (RAY1216 (150-600 mg/kg/day; i.g.; 5 days) effectively prolongs survival of SARS-CoV-2 infected mice.
Compound pharmacokinetics parameters in different animal species

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

C_max: the maximum observed concentration of the drug collected in bodily material from subjects in a clinical study
T_max: the time it takes to reach the maximum concentration or time to C_max
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
Vd_ss: Steady state volume of distribution
T_1/2: Half-time is the time it takes for half the drug concentration to be eliminated
oral (F%): Oral bioavailability

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