2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺
![2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺,210755-45-6,结构式](https://www.chemicalbook.com/CAS/GIF/210755-45-6.gif)
- CAS号:210755-45-6
- 英文名:CP 471,474
- 中文名:2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺
- CBNumber:CB61389258
- 分子式:C16H17FN2O5S
- 分子量:368.38
- MOL File:210755-45-6.mol
- 熔点 :135-137°C (dec.)
- 密度 :1.375±0.06 g/cm3(Predicted)
- 储存条件 :room temp
- 溶解度 :DMSO: ≥20mg/mL
- 酸度系数(pKa) :9.33±0.50(Predicted)
- 形态 :powder
- 颜色 :white to off-white
2-[[[4-(4-氟苯氧基)苯基]磺酰基]氨基] -N-羟基-2-甲基丙酰胺性质、用途与生产工艺
- 生物活性 CP-471474 是一个口服有效的、广泛的 MMP 抑制剂，IC50 值分别为1170 nM (MMP-1)、0.7 nM (MMP-2)、16 nM (MMP-3)、13 nM (MMP-9) 和 0.9 nM (MMP-13)。
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靶点
MMP-2
0.7 nM (IC 50 )
MMP-13
0.9 nM (IC 50 )
MMP-9
13 nM (IC 50 )
MMP-3
16 nM (IC 50 )
MMP-1
1170 nM (IC 50 )
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体内研究
CP-471474 plasma levels following subcutaneous injection are 2,020 ng/mL (1 h postdose) to 160 ng/mL (6 h postdose).
CP-471,474 significantly reduces both the extent and severity of inflammation at 2 months. At 4 months, a spontaneous reduction of the inflammatory response is observed in both treated and untreated animals, and consequently no difference is observed between both.
CP-471474 significantly decreases the destructive lesions mainly at 2 months and also at 4 months.
Animal Model: Guinea pigs weighing 400 to 450 g (COPD). Dosage: 20 mg/kg (also supplemented daily by the diet (200 mg/200 g powdered chow)). Administration: Subcutaneously (in 20% ethanol/80% polyethylene glycol), once a day during the entire course. Result: Lungs derived from smoking animals treated with the compound demonstrated a statistically significant reduction in the destructive lesions.
Showed an increase of both pro–MMP-9 and its active form (lanes 5 to 8) as compared with control animals.
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- 国家：印度
- 产品数：6257
- 优势度：58
