CES2A-IN-2 |
CES2A-IN-2 : Covalent Inhibitor of CES2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| CES2 |
|
|
Covalent Inhibitor
up to 10 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The selectivity of 14n toward hCES2A was evaluated using a panel of key human serine hydrolases, inc ...
Selectivity Assessment Description:
14n demonstrated relatively weak inhibition of hCES1A (IC50 = 4403 nM) and hBuChE (IC50 = 3063 nM), ...
Potency Cellular
In Vitro
CES2
Mode of Action: Covalent Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acs.jmedchem.4c02560
In Vivo Validations
Mouse
Dose: 100 mg/Kg
Route of delivery:
oral gavage
Target engagement assay:
No significant changes on body weight, mental state, or movement behaviors were observed. HE analysis showed that no abnormal findings or toxic symptoms in major organs, including the heart, liver, brain, lung, spleen, kidney, stomach and gastrointestinal tract (Figure 5B). Meanwhile, there were no significant changes in biochemical parameters (AST, ALT, ALB, ALP, TP, UREA, CREA) between 14n-treated mice (daily for 14 days) and the control group (Figure 5C–I). These findings clearly suggested that 14n possessed good safety profiles in mice.
DOI Reference: 10.1021/acs.jmedchem.4c02560
Chemical Information
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