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PF-152

Chemical Structure : PF-152

CAS No.: 1112169-64-8

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PF-152 (PF152)

Catalog No.: PC-61148Not For Human Use, Lab Use Only.

PF-152 is a potent, highly selective and orally bioavailable MMP13 inhibitor with Ki of 1.5 nM, with no activity against MMP3 (Ki>10 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PF-152 is a potent, highly selective and orally bioavailable MMP13 inhibitor with Ki of 1.5 nM, with no activity against MMP3 (Ki>10 uM).
PF-152 also displays high selectivity against a panel of 14 matrix metalloproteinases, TACE, ADAMTS-4 and ADAMTS-5.
PF-152 suppresses MMP-13 mediated cartilage degradation in vivo, shows potential for treatment of oteoarthritis.

Physicochemical Properties

M.Wt 473.465
Formula C21H24FN7O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide

References

1. Ruminski PG, et al. J Med Chem. 2016 Jan 14;59(1):313-27.

2. Settle S, et al. Arthritis Rheum. 2010 Oct;62(10):3006-15.

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