产品
编 号:F755888
分子式:C22H20Cl2N4O2S
分子量:475.39
产品类型
结构图
CAS No: 2768834-39-3
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产品详情
生物活性:
SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent Mpro inhibitor (IC50=0.40 μM) with good anti-SARS-CoV-2 activity (EC50=1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies.
体内研究:
SARS-CoV-2 Mpro-IN-2 (2 mg/kg; i.v.; single) exhibits clearance rate (CL), mean residence time (MRT), and half-life (t1/2) are 3140 mL/h/kg, 0.40 h, and 0.36 h, respectively.SARS-CoV-2 Mpro-IN-2 (10 mg/kg; p.o.; single) is rapidly absorbed, with a time-to-maximum concentration (Tmax) of 0.5 h, and shows a moderate pharmacokinetic profile including a favorable t1/2 (1.73 h), a maximum concentration (Cmax) 74.6 ng/mL, and an area under curve (AUC0-t) of 235 ng h/mL.Animal Model:Male Sprague-Dawley rats.
Dosage:2 mg/kg (for i.v.); 10 mg/kg (for p.o.).
Administration:Intravenous injection or oral administration; single.
Result:1.19Pharmacokinetic Parameters of SARS-CoV-2 Mpro-IN-2 in Male Sprague-Dawley rats.IV (2 mg/kg) PO (10 mg/kg)
t1/2 (h)0.361.73
Tmax (h)0.080.5
Cmax (ng/mL)131074.6
C0 (ng/mL)1760-
AUC0-t (ng/mL?h)627235
AUC0-∞ (ng/mL?h)637230
MRT0-∞ (h)0.402.45
CL (mL/h/kg)3140-
F (%)-7.2
体外研究:
SARS-CoV-2 Mpro-IN-2 (0.01-100 μM; 4 h) shows low cytotoxicity in Vero E6 cells.