BR351是可渗透血脑屏障的MMP抑制剂，抑制MMP2，MMP8，MMP9，MMP13的IC50分别为4，2，11，50nM。是正电子发射断层扫描成像活化MMP分子的潜在工具。
BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively[1]. Potential tools for the molecular imaging of activated MMPs with PET[2].
[18F]BR351 Is quickly metabolized in plasma with 20.28% ± 5.41% of intact tracer remaining at 15 minutes postinjection[2].
[1]. Wagner S, et al. Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET. J Med Chem. 2007 Nov 15;50(23):5752-64. [2]. Vazquez N, et al. Evaluation of [18 F]BR420 and [18 F]BR351 as radiotracers for MMP-9 imaging in colorectal cancer. J Labelled Comp Radiopharm. 2017 Jan;60(1):69-79.
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