Cathepsin inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
Cathepsin inhibitor 1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Vero-E6 cells
51.70 nM (14a), <40 nM (14b)
24 hours
Evaluate the inhibitory activity of 14a and 14b against authentic SARS-CoV-2 virus, results showed significant antiviral effects
Signal Transduct Target Ther. 2024 Mar 6;9(1):54.
Huh-7 cells
8.24 nM (14a), 10.06 nM (14b)
36 hours
Evaluate the inhibitory activity of 14a and 14b against other coronavirus pseudoviruses, results showed broad-spectrum antiviral effects
Signal Transduct Target Ther. 2024 Mar 6;9(1):54.
293T/ACE2 cells
3.33 nM (14a), 0.61 nM (14b)
36 hours
Evaluate the inhibitory activity of 14a and 14b against SARS-CoV-2 pseudovirus, results showed significant antiviral effects
Signal Transduct Target Ther. 2024 Mar 6;9(1):54.
Cathepsin inhibitor 1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Ovariectomized (OVX) osteoporotic mouse model
Oral
50 mg/kg body weight
Once daily for 30 days
Inhibition of cathepsin K increases preosteoclast numbers, resulting in higher levels of PDGF-BB to stimulate CD31hiEmcnhi vessels and bone formation in OVX mice
Nat Med. 2014 Nov;20(11):1270-8
K18-hACE2 transgenic mice
SARS-CoV-2 XBB 1.16 variant infection model
Intranasal administration
10 mg/kg and 20 mg/kg
Administered once at 24 h post infection
Evaluate the in vivo antiviral efficacy of 14a and 14b against SARS-CoV-2 XBB 1.16 variant, results showed significant reduction in lung viral load
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