1. Immunology/Inflammation
  2. COX
  3. COX-2-IN-61

COX-2-IN-61 是一种口服有效的 COX-2 抑制剂,IC50 为 22 µM,同时对 COX-1 也有抑制作用,IC50 为 43 µM。COX-2-IN-61 在 Carrageenan (HY-125474) 诱导的大鼠足爪水肿模型中表现出抗炎作用,且安全性良好。COX-2-IN-61 可用于炎症研究。

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COX-2-IN-61

COX-2-IN-61 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-61 is an orally active COX-2 inhibitor with an IC50 of 22 µM, also inhibits COX-1 with an IC50 of 43 µM. COX-2-IN-61 exhibits anti-inflammation effects in a Carrageenan (HY-125474) induced rat paw edema model, with promising safety profiles. COX-2-IN-61 can be used for the research of inflammation[1].

IC50 & Target[1]

COX-1

43 μM (IC50)

COX-2

22 μM (IC50)

体外研究
(In Vitro)

COX-2-IN-61 (compound 4) 与 Arg513 和 Ala527 形成氢键,并与 Val523、Met522 和 Val349 形成疏水相互作用,这有助于其与 COX-2 结合并发挥抗炎作用[1]

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

体内研究
(In Vivo)

COX-2-IN-61 (compound 4) (50 mg/kg,口服,单次给药) 在 Carrageenan 诱导的大鼠爪水肿模型中表现出显著的抗炎活性,与 Celecoxib (HY-14398) 活性相当[1]
COX-2-IN-61 (50 mg/kg,口服,每日一次,持续 14 天) 与 Celecoxib 相比,在大鼠中显示出较低的致溃疡性、心脏毒性和肾毒性[1]

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

Animal Model: Male Wistar rats (180-225 g) induced by Carrageenan (1%, 1 mL) injection[1]
Dosage: 50 mg/kg
Administration: p.o., single dose
Result: Showed significant anti-inflammatory activity, with 47% edema inhibition at 6 hours.
Demonstrated equal anti-inflammatory activity to Celecoxib after 4h interval.
Animal Model: Male Wistar rats (180-225 g)[1]
Dosage: 50 mg/kg
Administration: p.o., daily for 14 days
Result: Markedly reduced histopathological damage of the stomach, heart, and kidney, compared to Celecoxib.
Resulted in a significantly lower increase in cardiac biomarkers (CK-MB, troponin I, AST, LDH) and renal injury biomarkers (creatinine, urea), compared to Celecoxib.
分子量

347.41

Formula

C15H13N3O3S2

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-61
目录号:
HY-179700
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