230961-08-7
230961-08-7 结构式
基本信息
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
物理化学性质
常见问题列表
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MMP-3 5.9 nM (IC 50 ) |
MMP-13 73 nM (IC 50 ) |
MMP-9 0.84 μM (IC 50 ) |
MMP-2 1.79 μM (IC 50 ) |
MMP-14 1.9 μM (IC 50 ) |
MMP-1 51 μM (IC 50 ) |
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.
| Animal Model: | Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO) |
| Dosage: | 15 mg/kg |
| Administration: | Intravenous injection; for 24 h or 7 days |
| Result: | Significantly reduced MMP3 activity in the brain. |