UK 356618
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- CAS号:
- 230961-08-7
- 英文名:
- N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine
- 英文别名:
- UK 356618;PF-03890101;UK 356618 - PF 03890101;N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine;(2R)-N1-[(1S)-2,2-Dimethyl-1-({[(1R)-1-phenylethyl]amino}carbonyl)propyl]-2-{3-[(3-methyl-4-phenyl)-phenyl]propyl}-(N4-hydroxy)butanediamide;(2R)-N1-[(1S)-2,2-DiMethyl-1-[[[(1R)-1-phenylethyl]aMino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-Methyl[1,1'-biphenyl]-4-yl)propyl]butanediaMide;Butanediamide, N1-[(1S)-2,2-dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-, (2R)-
- 中文名:
- UK 356618
- 中文别名:
- 化合物 T17201
- CBNumber:
- CB82518853
- 分子式:
- C34H43N3O4
- 分子量:
- 557.72
- MOL File:
- 230961-08-7.mol
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UK 356618化学性质
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熔点:
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93-102oC
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密度:
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1.124±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: ≥25mg/mL
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形态:
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powder
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酸度系数(pKa):
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9.16±0.20(Predicted)
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颜色:
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white to tan
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旋光性 (optical activity):
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[α]/D >+25.0°, c = 0.5 in methanol
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UK 356618性质、用途与生产工艺
UK 356618 (Compound 4j) 是一种有效且选择性的基质金属蛋白酶 3 (MMP-3) 抑制剂，其 IC50 值为 5.9 nM。与 MMP-3相比，UK 356618 对 MMP-1，MMP-2，MMP-9， MMP-13 和 MMP-14 的抑制效力较低。
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MMP-3
5.9 nM (IC
50
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MMP-13
73 nM (IC
50
)
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MMP-9
0.84 μM (IC
50
)
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MMP-2
1.79 μM (IC
50
)
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MMP-14
1.9 μM (IC
50
)
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MMP-1
51 μM (IC
50
)
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Inhibition of MMP-3 and selectivity over MMP-2 was remarkably sensitive to the size of the substituent and is clearly optimal for a methyl group (UK 356618, compound 4j). UK 356618 is more widely profiled against other MMPs.
MMP-13 is closely involved in IL-6 or TNF-α increasing tumor metastasis. MMP-13 deficiency abrogate TNF-α effect on lung cancer cell migration. UK 356618 treatment efficiently abolished the effect of TNF-α on cell migration in NCI-H446 cells.
UK 356618 (15 mg/kg; intravenous injection; for 24 h or 7 days; male Wistar rats) treatment at reperfusion significantly reduces MMP3 activity in the brain.
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Animal Model:
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Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO)
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Dosage:
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15 mg/kg
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Administration:
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Intravenous injection; for 24 h or 7 days
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Result:
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Significantly reduced MMP3 activity in the brain.
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UK 356618
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-107394 | UK 356618
UK 356618 | 230961-08-7 | 1mg | 1700元 |
| 2024/04/30 | HY-107394 | UK 356618 | | 10 mM * 1 mLin DMSO | 5610元 |
230961-08-7, UK 356618 相关搜索:
- Pharmaceuticals
- Pfizer Compounds
- Intermediates & Fine Chemicals
- Inhibitors
- Heterocycles
- Aromatics
- C34H43N3O4
- 化合物 T17201
- 230961-08-7
- Butanediamide, N1-[(1S)-2,2-dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-, (2R)-
- UK 356618
- UK 356618 - PF 03890101
- (2R)-N1-[(1S)-2,2-Dimethyl-1-({[(1R)-1-phenylethyl]amino}carbonyl)propyl]-2-{3-[(3-methyl-4-phenyl)-phenyl]propyl}-(N4-hydroxy)butanediamide
- PF-03890101
- (2R)-N1-[(1S)-2,2-DiMethyl-1-[[[(1R)-1-phenylethyl]aMino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-Methyl[1,1'-biphenyl]-4-yl)propyl]butanediaMide
- N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine