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BR351

Names

[ CAS No. ]:
960113-85-3

[ Name ]:
BR351

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[Target]

MMP-9:11 nM (IC50)

MMP-2:4 nM (IC50)

MMP-8:2 nM (IC50)

MMP13:50 nM (IC50)


[In Vivo]

[18F]BR351 Is quickly metabolized in plasma with 20.28% ± 5.41% of intact tracer remaining at 15 minutes postinjection[2].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H25FN2O5S

[ Molecular Weight ]:
424.49

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds