1. Immunology/Inflammation Apoptosis
  2. COX TNF Receptor Interleukin Related
  3. 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.

For research use only. We do not sell to patients.

COX-2-IN-60

COX-2-IN-60 Chemical Structure

CAS No. : 3073624-74-2

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Description

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[1].

IC50 & Target[1]

COX-2

0.06 μM (IC50)

COX-1

5.93 μM (IC50)

In Vitro

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.

In Vivo

COX-2-IN-60 (compound 7b) (20 mg/kg, p.o., 30 min pre-Pilocarpine) exhibits significant anticonvulsant effects and protects against hippocampal injury by suppressing oxidative stress, pro-ininammatory signaling, and glial activationin in the Pilocarpine (HY-B0726A)-induced seizure mouse model[1].
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.

Animal Model: Pilocarpine (HY-B0726A)-induced seizure model[1]
Dosage: 20 mg/kg
Administration: p.o., 30 min pre-Pilocarpine
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.
Molecular Weight

391.22

Formula

C17H15BrN2O4

CAS No.
SMILES

O=C(O)COC1=CC=C(Br)C=C1/C=N/NC(CC2=CC=CC=C2)=O

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
COX-2-IN-60
Cat. No.:
HY-179142
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