COX-2/sEH-IN-1
COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks.
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- CAS No.: 2474977-38-1
- Formule: C23H18F3N5O3S
- Masse moléculaire:501.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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sEH 0.40 nM (IC50) |
COX-2 1.24 μM (IC50) |
COX-1 8.72 μM (IC50) |
In Vivo
COX-2/sEH-IN-1 (50 mg/kg; p.o.; once) shows high anti-inflammatory activity[1].
COX-2/sEH-IN-1 (100 mg/kg; p.o.; 2 weeks) affords a perfect cardio-protection and less cardiovascular liabilities[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino mice (20-30 g)[1]
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Dosage:10 mg/kg
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Administration:Oral administration, once
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Result:Exhibited analgesic activity with 65.67% inhibition in the number of writhing.
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Animal Model:Albino rats (120-150 g), carrageenan-induced paw edema model[1]
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Dosage:50 mg/kg
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Administration:Oral administration, once
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Result:Showed high anti-inflammatory activity with edema inhibition of 64.06%, 95.82%, and 98.15% at 1, 3, 5 h, respectively.
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Animal Model:Adult male albino Wister rats (170-200 g)[1]
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Dosage:100 mg/kg
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Administration:Oral administration, 2 weeks
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Result:Exhibited a significant lowering in Troponine-I, LDH and CK-MB levels when compared to celecoxib treated group. Showed remarkably decrease in TNF-α concentration compared to the celecoxib induced cardio-toxicity group. Restored heart GSH level and significantly increased PGI2 level compared to celecoxib group. Showed mild decongestant and mild edema on cardiac blood vessels and showed more or less normal muscle bundles.
Chemical Information
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CAS No. 2474977-38-1
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Masse moléculaire 501.48
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Formule C23H18F3N5O3S
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SMILES
NS(=O)(C1=CC=C(C=C1)N2N=C(C=C2C3=CC=CC=C3)NC(NC4=CC=C(C=C4)C(F)(F)F)=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)
COX-2/sEH-IN-1 Related Classifications
HY-146704 Related Classifications
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