For research use only. Not for therapeutic Use.
PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771[1][2].
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].
PF-05198007 (1 or 10 mg/kg, orally) reduces the capsaicin flare response in WT, but not Nav1.7Nav1.8Cre mice[1].
| Catalog Number | I016393 |
| CAS Number | 1235406-19-5 |
| Synonyms | 4-[2-(5-amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide |
| Molecular Formula | C19H12ClF4N5O3S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H12ClF4N5O3S2/c20-12-4-16(34(30,31)29-17-7-33-8-26-17)13(21)5-15(12)32-14-2-1-9(19(22,23)24)3-10(14)11-6-27-28-18(11)25/h1-8,29H,(H3,25,27,28) |
| InChIKey | QCDLGAPJZJODRJ-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C=C1C(F)(F)F)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F |
| Reference | [1]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. [2]. Kushnarev M, et al. Neuropathic pain: preclinical and early clinical progress with voltage-gated sodium channel blockers. Expert Opin Investig Drugs. 2020 Mar;29(3):259-271. |
