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Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $2,428 | Backorder |
Description | Nav1.7-IN-8 is a highly potent and selective inhibitor of NaV1.7, exhibiting greater selectivity for inhibiting NaV1.7 compared to the subtypes hNaV1.1 and hNaV1.5. Additionally, Nav1.7-IN-8 has inhibitory effects on CYP2C9 and CYP3A4, with IC50 values of 0.17 μM and 0.077 μM, respectively. Notably, Nav1.7-IN-8 demonstrates significant analgesic properties in rodent models of both acute and inflammatory pain. |
Targets&IC50 | CYP2C9:0.17 μM (IC50), CYP3A4:0.077 μM (IC50) |
In vitro | The plasma protein binding of Nav1.7-IN-8 in rats is extremely high, with a free fraction of approximately 1.1% [1]. |
In vivo | Nav1.7-IN-8, administered intraperitoneally (i.p.) at doses ranging from 0 to 100 mpk for one hour, significantly reduces the pain response during phase 2a of the formalin assay in both rats and mice in a dose-dependent manner. Furthermore, when administered at 10 to 100 mpk over two days, it demonstrates a consistent dose-dependent decrease in pain response across these animal models, indicating its potential as an effective analgesic[1]. |
Alias | Nav1.7-IN-8 |
Molecular Weight | 535.93 |
Formula | C21H12ClF2N5O4S2 |
Cas No. | 1432913-44-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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