PF-05198007
Names
[ CAS No. ]:
1235406-19-5
[ Name ]:
PF-05198007
Biological Activity
[Description]:
PF-05198007 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 9 nM, no significant activity against Nav1.5 (IC50>10 uM); increases action potential rheobase in small diameter mDRG neurons, demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.
[Related Catalog]:
[Target]
Nav1.7[1].
[In Vitro]
PF-05198007 (30 nM) blocks on average 83.0 ± 2.7% of the total TTX-S current indicating that the major TTX-S conductance is carried through Nav1.7 channels in small-diameter mouse DRG neurons (n = 35)[1].
[In Vivo]
PF-05198007 (1 or 10 mg/kg, orally) reduces the capsaicin flare response in WT, but not Nav1.7Nav1.8Cre mice[1]. Animal Model: Adult Male C57Bl/6J Wild type (WT) and Nav1.7Nav1.8Cre mice[1]. Dosage: 1 or 10 mg/kg. Administration: Orally once. Result: Reduced the flare response to capsaicin for the duration of the observation period (55 mins; Vehicle; 4930 ± 751 versus 1 and 10 mg/kg 1967 ± 472 and 2265 ± 382, respectively (n = 7), AUC, p < 0.05).
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C19H12ClF4N5O3S2
[ Molecular Weight ]:
533.901