2. Immunology/Inflammation Apoptosis
  3. COX TNF Receptor Interleukin Related
  4. COX-2-IN-60

COX-2-IN-60 是一种强效、具有口服活性且选择性 COX-2 抑制剂，其 IC50 值为 0.06 μM。COX-2-IN-60 对 COX-2 的选择性约为 COX-1 (IC50 = 5.93 μM) 的 100 倍。COX-2-IN-60 能够减少氧化应激和神经炎症细胞因子，并有效对抗癫痫发生。COX-2-IN-60 在 Pilocarpine (HY-B0726A) 诱导的小鼠癫痫模型中，表现出显著的抗惊厥作用，并通过抑制氧化应激 (降低 MDA 和 NO 水平)、促炎信号 (降低 TNF-α 和 IL-6 水平) 以及神经胶质细胞活化，来保护海马体免受损伤。COX-2-IN-60 可用于神经炎症和癫痫的相关研究。

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COX-2-IN-60

COX-2-IN-60 Chemical Structure

CAS No. : 3073624-74-2

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COX-2-IN-60 相关抗体

Top Publications Citing Use of Products

查看 COX 亚型特异性产品:

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COX COX-1 COX-2 COX-3

查看 TNF Receptor 亚型特异性产品:

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

COX-2-IN-60 (compound 7b) 不仅像 Valproic acid (HY-10585) 一样与 Thr29、Val289 和 Arg119 形成关键氢键，而且还通过其苯氧基与 Thr333 以及其腙羰基与 Tyr193 建立额外的键，从而实现优异的结合稳定性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

COX-2-IN-60 相关抗体:
体内研究
(In Vivo)

COX-2-IN-60 (compound 7b) (20 mg/kg，口服，于 Pilocarpine 前 30 分钟给药) 在 Pilocarpine (HY-B0726A) 诱发的癫痫小鼠模型中表现出显著的抗惊厥作用，并通过抑制氧化应激、促炎信号传导和胶质细胞活化[1]。
COX-2-IN-60 在 Pentylenetetrazol (PTZ) 诱导的小鼠急性癫痫模型中，可完全抑制癫痫发作，且无动物死亡[1]。

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.
分子量

391.22

Formula

C17H15BrN2O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

COX-2-IN-60 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

COX-2-IN-603073624-74-2COXTNF ReceptorInterleukin RelatedCyclooxygenaseTumor Necrosis Factor ReceptorTNFRILreduced oxidative stress,downregulated glial activation,suppressed neuroinflammatory cytokines,seizure protection,safe multifunction candidate,compound 7b,anti-inflammatory activity,attenuated excitotoxic glutamateInhibitorinhibitorinhibit

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