N-(3-pyridyl)-Indomethacin amide
- 品牌：APExBIO
- 型号：5mg/10mg/50mg
- 供应商：上海伟寰生物科技有限公司
- 供应商报价：￥767 - 5915
- 标签：N-(3-pyridyl)-Indomethacin amide、N-(3-pyridyl)-Indomethacin amide价格、N-(3-pyridyl)-Indomethacin amide厂家、、APExBIO、上海伟寰生物科技有限公司
产品库
| 规格： | 5mg | 产品价格： | ￥767.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥1352.0 |
| 规格： | 50mg | 产品价格： | ￥5915.0 |
| CAS号 | 261766-29-4 | ||
| 别名 | N-3PyIA | ||
| 分子式 | C24H20ClN3O3 | 分子量 | 433.9 |
| 溶解性 | Soluble in DMSO | 储存条件 | Store at -20° |
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N-(3-pyridyl)-Indomethacin amide is a reversible, potent and selective COX-2 inhibitor [1].
Cyclooxygenase (COX) is an enzyme responsible for formation of prostanoids, including thromboxane and prostaglandins such as prostacyclin. COX-1 is the constitutive isoform and is mainly responsible for the synthesis of cytoprotective prostaglandins in the gastrointestinal tract (GI) and of the proaggregatory thromboxane in blood platelets. COX-2 is inducible and short-lived that is stimulated by endotoxin, cytokines, and mitogens. COX-2 plays important roles in prostaglandin biosynthesis in inflammatory cells the central nervous system [1].
N-(3-pyridyl)-indomethacin amide (N-3PyIA) is a reversible, potent and selective COX-2 inhibitor that inhibits human recombinant COX-2 and ovine COX-1 with IC50 values of 0.052 and >66 μM, respectively. It is over 1300 times less potent as an inhibitor of ovine COX-1. N-(3-pyridyl)-indomethacin amide is the 3-pyridyl amide derivative of indomethacin that shows selective against COX-2 [1].
Reference:
[1]. Kalgutkar AS, Marnett AB, Crews BC, et al. Ester and amide derivatives of the nonsteroidal antiinflammatory drug, indomethacin, as selective cyclooxygenase-2 inhibitors. J Med Chem. 2000 Jul 27;43(15):2860-70.
