产品
编 号：F745153
分子式：C21H12ClF2N5O4S2
分子量：535.93
分子式：C21H12ClF2N5O4S2
分子量：535.93
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CAS No: 1432913-44-4
产品详情
生物活性：
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.
体内研究：
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..Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response.Animal Model:Rats
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
Dosage:10~100 mpk
Administration:I.p.; 2 days
Result:Displayed a dose-dependent reduction of the pain response.
体外研究：
Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ～1.1 %.
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.
体内研究：
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..Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response.Animal Model:Rats
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
Dosage:10~100 mpk
Administration:I.p.; 2 days
Result:Displayed a dose-dependent reduction of the pain response.
体外研究：
Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ～1.1 %.
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