SARS-CoV-2 Mpro-IN-2 (化合物 GC-14) 是一种选择性的、低细胞毒性的非共价Mpro抑制剂(IC50=0.40 μM)，具有良好的抗 SARS-CoV-2 活性 (EC50=1.1 μM)。SARS-CoV-2 Mpro-IN-2 可用于 COVID-19 的研究。

SARS-CoV-2 Mpro-IN-2 (compound GC-14) is a selective, low cytotoxic and non-covalent M pro inhibitor ( IC 50 =0.40 μM) with good anti-SARS-CoV-2 activity ( EC 50 =1.1 μM). SARS-CoV-2 Mpro-IN-2 can be used in COVID-19 studies [1].

SARS-CoV-2 Mpro-IN-2 (0.01-100 μM; 4 h) shows low cytotoxicity in Vero E6 cells [1]. Cell Cytotoxicity Assay [1] Cell Line: Vero E6 cells Concentration: 0.01-100 μM Incubation Time: 4 h Result: Exhibited low cytotoxicity with a CC 50 value of more than 100 μM.

SARS-CoV-2 Mpro-IN-2 (2 mg/kg; i.v.; single) exhibits clearance rate (CL), mean residence time (MRT), and half-life (t 1/2 ) are 3140 mL/h/kg, 0.40 h, and 0.36 h, respectively [1]. SARS-CoV-2 Mpro-IN-2 (10 mg/kg; p.o.; single) is rapidly absorbed, with a time-to-maximum concentration (T max ) of 0.5 h, and shows a moderate pharmacokinetic profile including a favorable t 1/2 (1.73 h), a maximum concentration (C max ) 74.6 ng/mL, and an area under curve (AUC 0-t ) of 235 ng h/mL [1]. Animal Model: Male Sprague-Dawley rats [1]. Dosage: 2 mg/kg (for i.v.); 10 mg/kg (for p.o.). Administration: Intravenous injection or oral administration; single. Result: 1.19 Pharmacokinetic Parameters of SARS-CoV-2 Mpro-IN-2 in Male Sprague-Dawley rats [1]. IV (2 mg/kg) PO (10 mg/kg) t 1/2 (h) 0.36 1.73 T max (h) 0.08 0.5 C max (ng/mL) 1310 74.6 C 0 (ng/mL) 1760 - AUC 0-t (ng/mL h) 627 235 AUC 0-∞ (ng/mL h) 637 230 MRT 0-∞ (h) 0.40 2.45 CL (mL/h/kg) 3140 - F (%) - 7.2

2768834-39-3

C22H20Cl2N4O2S

475.39

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years