产品
编 号:F085350
分子式:C18H12Cl2FN5O3S2
分子量:500.35
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7,ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.

体外研究:
PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4).PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5, Fig 5D) whilst 100 nM resulted in complete block.
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