CES2A-IN-4
CES2A-IN-4 is an orally active, time-dependent, irreversible, and selective CES2A inhibitor (hCES2A: IC50 value of 6.87 nM after 3 min preincubation, and IC50 value of 0.052 nM after 33 min preincubation). CES2A-IN-4 attenuates Irinotecan (HY-16562)-induced inflammation by reducing IL-6 and ROS levels and maintaining mitochondrial membrane potential.
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- Formule: C19H17NO6
- Masse moléculaire:355.34
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
IL-6 |
hCES1A 55.34 nM (IC50) |
hCES2A 0.052 nM (IC50) |
In Vitro
CES2A-IN-4 (1 μM) shows acceptable selectivity for hCES2A over other serine hydrolases, with approximately 39-fold selectivity over hCES1A[1].
CES2A-IN-4 (0-15 nM; 0-36 min) covalently modifies the catalytic Ser-228 and inactivates hCES2A, with KI = 2.50 nM[1].
CES2A-IN-4 (1 h) inhibits hCES2A activity in HepG2 cells[1].
CES2A-IN-4 (3 μM; 1 h) inhibits hCES2A activity in intestinal organoids[1].
CES2A-IN-4 dose-dependently protects NCM460 colonic epithelial cells from Irinotecan-induced cytotoxicity[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/6 (male)[1]
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Dosage:25 mg/kg/d; 50 mg/kg/d
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Administration:intragastric (i.g.); daily; for 14 days
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Result:Reduced disease activity index scores, alleviated irinotecan-induced body weight loss and diarrhea, and prevented colon shortening.
Preserved intestinal crypt and villus architecture, increased goblet cell mucus secretion, and upregulated claudin-1 expression in colonic tissue.
Reduced colonic SN-38 exposure and decreased colonic levels of TNF-α, IL-1β, and IL-6.
High-dose restored irinotecan-elevated serum ALT, AST, and CREA toward near-normal levels.
Tumor-bearing mice maintained irinotecan antitumor efficacy.
Chemical Information
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Masse moléculaire 355.34
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Formule C19H17NO6
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SMILES
CCN(C)C(OC1=CC2=C(C(O)=C1)C(C=C(C3=CC=C(O)C=C3)O2)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CES2A-IN-4 Related Classifications
HY-190794 Related Classifications
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Keywords
- CES2A-IN-4
- Carboxylesterase (CES)
- Reactive Oxygen Species (ROS)
- Interleukin Related
- Mitochondrial Metabolism
- Carboxylesterase
- Carboxylic-ester Hydrolase
- IL
- HepG2 cells
- carbamate
- catalytic serine
- colon epithelial cells
- hCES2A
- intestinal organoids
- irinotecan-induced intestinal toxicity
- pro-inflammatory cytokine production
- reactive oxygen species
- serine hydrolase
- Inhibitor
- inhibitor
- inhibit