1235406-19-5
1235406-19-5 structure
- Name: PF-05198007
- Chemical Name: PF-05198007
- CAS Number: 1235406-19-5
- Molecular Formula: C19H12ClF4N5O3S2
- Molecular Weight: 533.901
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
- Create Date: 2020-01-19 12:02:04
- Modify Date: 2024-01-11 19:43:33
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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.
| Name | PF-05198007 |
|---|
| 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. |
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| 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 |
| Molecular Formula | C19H12ClF4N5O3S2 |
|---|---|
| Molecular Weight | 533.901 |