Carboxylesterase 2-IN-2
Carboxylesterase 2-IN-2 is an orally effective, potent, and selective Carboxylesterase 2 (CES2) inhibitor with an IC50 of 0.63 μM and a Ki of 0.98 μM. Carboxylesterase 2-IN-2 acts as a reversible competitive inhibitor that forms a hydrogen bond network with key residues in the active pocket of CES2, effectively occupying and blocking the catalytic active site of the enzyme, thereby ameliorating abnormal lipid accumulation. Carboxylesterase 2-IN-2 can be used for research on high-fat diet-induced obesity and lipid metabolism disorders.
For research use only. We do not sell to patients.
- Formula: C24H17NO7
- Molecular Weight:431.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
hCES2 0.63 μM (IC50) |
hCES2 0.98 μM (Ki) |
In Vitro
Carboxylesterase 2-IN-2 (30 min) is a potent, reversible competitive CES2 inhibitor with an IC50 of 0.63 μM and a Ki of 0.98 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-week-old)[1]
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Dosage:25 mg/kg body weight/day; 100 mg/kg body weight/day
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Administration:i.g.; once daily; 5 weeks
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Result:Significantly and dose-dependently inhibited the excessive body weight gain induced by HFD and reduced the weight of epididymal adipose tissue.
Improved hepatic hypertrophy; H&E and Oil Red O staining confirmed it effectively cleared lipid vacuoles in hepatocytes and reversed hepatic steatosis (fatty liver).
Comprehensively improved the serum lipid profile state by significantly decreasing triglyceride (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-C) levels, while maintaining/improving high-density lipoprotein cholesterol (HDL-C) levels.
Reduced the elevated levels of liver injury markers AST and ALT in serum, demonstrating a protective effect on the liver.
Chemical Information
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Molecular Weight 431.39
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Formula C24H17NO7
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SMILES
COC1=CC=C(C=C1)[C@H]2C3=C4OC(C5=CC=CC=C5)=CC(C4=C(C=C3O[C@@H]2[N+]([O-])=O)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)