230961-21-4
230961-21-4 结构式
基本信息
(R)-3-((S)-1-((S)-2-Methoxy-1-phenylethylaMino)-3,3-diMethyl-1-o
(R)-3-(((S)-1-(((S)-2-Methoxy-1-phenylethyl)amino)-3,3-dimethyl-1-oxobutan-2-yl)carbamoyl)-6-(2-m
(R)-3-((S)-1-((S)-2-methoxy-1-phenylethylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamoyl)-6-(2-methylbiphenyl-4-yl)hexanoic acid
(3R)-3-[[(2S)-1-[[(1S)-2-methoxy-1-phenylethyl]amino]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]-6-(3-methyl-4-phenylphenyl)hexanoic acid
(βR)-β-[[[(1S)-1-[[[(1S)-2-Methoxy-1-phenylethyl]amino]carbonyl]-2,2-dimethylpropyl]amino]carbonyl]-2-methyl-[1,1'-biphenyl]-4-hexanoicacid
[1,1'-Biphenyl]-4-hexanoic acid, β-[[[(1S)-1-[[[(1S)-2-methoxy-1-phenylethyl]amino]carbonyl]-2,2-dimethylpropyl]amino]carbonyl]-2-methyl-, (βR)-
物理化学性质
常见问题列表
|
MMP-3 23 nM (IC 50 ) |
MMP-12 42 nM (IC 50 ) |
MMP-8 1.75 μM (IC 50 ) |
MMP-13 2.3 μM (IC 50 ) |
MMP-7 5.8 μM (IC 50 ) |
MMP-9 30.4 μM (IC 50 ) |
MMP-2 34.2 μM (IC 50 ) |
MMP-14 66.9 μM (IC 50 ) |
The potency of UK-370106 (compound 7) for the inhibition of MMP-13 is 2.3 µM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC
50
> 100 µM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC
50
of 34.2 µM), MMP-7 (IC
50
of 5.8 µM), MMP-8 (IC
50
of 1.75 µM), MMP-9 (IC
50
of 30.4 µM) and MMP-14 (IC
50
of 66.9 µM).
UK-370106 potently inhibits cleavage of [
3
H]-fibronectin by MMP-3 (IC
50
of 320 nM) but does not inhibit cleavage of [
3
H]-gelatin by either MMP-2 or -9 up to the highest concentration tested (100 µM).
UK-370106 is not cytotoxic to, nor affected proliferation of, fibroblasts, keratinocytes, or endothelial cells at 50-100 µM in vitro.
Following iv (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is cleared rapidly (t 1/2 = 23 min) from plasma, but slowly (t 1/2 approximately 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo.