| Bioactivity | 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | PF-05198007 | ||||||||||||
| CAS | 1235406-19-5 | ||||||||||||
| Formula | C19H12ClF4N5O3S2 | ||||||||||||
| Molar Mass | 533.91 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
PF-05198007
CAS: 1235406-19-5 F: C19H12ClF4N5O3S2 W: 533.91
PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a
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