1432913-44-4
1432913-44-4 structure
- Name: Nav1.7-IN-8
- Chemical Name: Nav1.7-IN-8
- CAS Number: 1432913-44-4
- Molecular Formula: C21H12ClF2N5O4S2
- Molecular Weight: 535.93
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
- Create Date: 2021-09-10 11:34:58
- Modify Date: 2024-04-09 18:13:33
-
Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1].
| Name | Nav1.7-IN-8 |
|---|
| Description | Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1]. |
|---|---|
| Related Catalog | |
| Target |
CYP2C9:0.17 μM (IC50) CYP3A4:0.077 μM (IC50) |
| In Vitro | Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %[1]. |
| In Vivo | Nav1.7-IN-8 (0~100 mpk, i.p.; 1 hour) shows a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produces a substantial inhibition of the pain response[1]. .Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response[1]. Animal Model: Rats[1] Dosage: 0~100 mpk Administration: I.p.; 1 hour Result: Showed a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produced a substantial inhibition of the pain response. Animal Model: Mice[1] Dosage: 10~100 mpk Administration: I.p.; 2 days Result: Displayed a dose-dependent reduction of the pain response. |
| References |
| Molecular Formula | C21H12ClF2N5O4S2 |
|---|---|
| Molecular Weight | 535.93 |