1. Immunology/Inflammation
  2. COX MyD88
  3. COX-2-IN-57

COX-2-IN-57 是一种具有口服活性的 COX-2 抑制剂,IC50 值为 0.02 μM。COX-2-IN-57 在 Cisplatin (HY-17394)/辐射诱导的神经病变大鼠模型中减少 MyD88 表达,并降低血清中 COX-2PGE2COX-1 水平。COX-2-IN-57 在热板、冷痛过敏和 Randall-Selitto 测试中显示出优异的镇痛效果,并具有肝/肾保护作用。COX-2-IN-57 可用于研究炎症。

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COX-2-IN-57

COX-2-IN-57 Chemical Structure

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查看 COX 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

COX-2-IN-57 is an orally active COX-2 inhibitor with an IC50 value of 0.02 μM. COX-2-IN-57 reduces MyD88 expression and decreases serum levels of COX-2, PGE2, and COX-1 in Cisplatin (HY-17394)/radiation-induced neuropathy rat model. COX-2-IN-57 demonstrates superior antinociceptive efficacy in hot plate, cold allodynia, and Randall-Selitto tests, along with hepato-/renal protection. COX-2-IN-57 can be used for the study of inflammation[1].

IC50 & Target[1]

COX-2

0.02 μM (IC50)

COX-1

 

体内研究
(In Vivo)

COX-2-IN-57 (Compound 16) (20 mg/kg,口服,一次) 在 Carrageenan (HY-125474) 诱导的雌性 Wistar 大鼠足爪水肿和痛觉过敏模型中显示双重抗炎和镇痛效果[1]
COX-2-IN-57 (20 mg/kg,口服,连续给药 5 天) 显著抑制 Cisplatin/γ-射线诱导的大鼠炎症模型中的炎症[1]

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

Animal Model: Carrageenan-induced paw edema and hyperalgesia model: 1% carrageenan solution (0.1 mL) was subcutaneously injected into the sub-plantar region of female Wistar rats to induce paw edema and hyperalgesia[1]
Dosage: 20 mg/kg
Administration: p.o., once
Result: Reduced paw edema increase percentage to 33.1% and elevated nociceptive threshold to 57 g.
Animal Model: Cisplatin/γ-ray-induced inflammation and neuropathic pain model: Female Wistar rats (120-150 g) were intraperitoneally injected with cisplatin (2 mg/kg) to induce pain, and exposed to 4 Gy sublethal dose of γ-rays on the 4th day of the experiment to establish the model[1]
Dosage: 20 mg/kg
Administration: p.o., continuous administration for 5 days
Result: Decreased serum COX-2 level, serum PGE2 level and serum COX-1 level.
Increased latency time to hot stimulation, latency time to cold stimulation and paw withdrawal force under mechanical pressure.
Suppressed spinal MyD88 expression.
Showed apparently normal neurons in spinal grey matter with mild gliosis and slight vacuolation in spinal white matter.
分子量

640.54

Formula

C34H23Cl2N3O4S

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
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  • 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.

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产品名称:
COX-2-IN-57
目录号:
HY-175637
需求量: