COX-2-IN-60
COX-2-IN-60 is a potent, orally active, and selective COX-2 inhibitor with an IC50 of 0.06 μM. COX-2-IN-60 exhibits ~100-fold selectivity over COX-1 (IC50 = 5.93 ). COX-2-IN-60 reduces oxidative stress and neuroinflammatory cytokines, and effectively counteracts epileptogenesis. COX-2-IN-60 exhibits significant anticonvulsant effects and protects against hippocampal injury by suppressing oxidative stress (reducing MDA and NO), pro-inflammatory signaling (reducing TNF-α and IL-6), and glial activationin in the Pilocarpine (HY-B0726A)-induced seizure mouse model. COX-2-IN-60 can be used for the research on neuroinflammatory and epilepsy.
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- CAS. Nr.: 3073624-74-2
- Formel: C17H15BrN2O4
- Molecular Weight:391.22
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Speicherung:
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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Chemical Information
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Biologische Aktivität
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COX-2 0.06 μM (IC50) |
COX-1 5.93 μM (IC50) |
COX-2-IN-60 (compound 7b) not only forms key hydrogen bonds with Thr29, Val289, and Arg119 like Valproic acid (HY-10585), but also establishes additional bonds via its phenoxy group with Thr333 and its hydrazone carbonyl with Tyr193, thereby achieving superior binding stability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
COX-2-IN-60 suppresses seizure and achieves complete protection with no observed mortality in the Pentylenetetrazol (PTZ)-induced acute seizure mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pilocarpine (HY-B0726A)-induced seizure model[1]
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Dosage:20 mg/kg
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Administration:p.o., 30 min pre-Pilocarpine
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Result:Produced significant anticonvulsant effect. Prolonged the latency to stage 3 seizures by 188.6%. Significantly attenuated seizure progression. Significantly reduced MDA and nitrite levels by 67.15% and 41.01%, respectively. Significantly reduced cytokines by 56.95% (TNF-a) and 62.97% (IL-6). effectively mitigated excitotoxicity, as indicated by a 61.5% reduction in hippocampal glutamate levels. Downregulated glial fibrillary acidic protein (GFAP), and ionized calcium-binding adapter molecule 1 (Iba-1) by 73.91% and 49.79%, respectively.
Chemical Information
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CAS. Nr. 3073624-74-2
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Molecular Weight 391.22
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Formel C17H15BrN2O4
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SMILES
O=C(O)COC1=CC=C(Br)C=C1/C=N/NC(CC2=CC=CC=C2)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
COX-2-IN-60 Related Classifications
HY-179142 Related Classifications
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