产品
编 号：F197775
分子式：C25H16ClF2N3O5S
分子量：543.93
分子式：C25H16ClF2N3O5S
分子量：543.93
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CAS No: 1642112-31-9
产品详情
生物活性：
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM.
体内研究：
AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior.Animal Model:CD-1 male mice
Dosage:30 or 100 mg/kg body weight
Administration:Oral
Result:Showed a dose-dependent reduction in overall nociceptive behavior.
体外研究：
AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons.The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM.
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM.
体内研究：
AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior.Animal Model:CD-1 male mice
Dosage:30 or 100 mg/kg body weight
Administration:Oral
Result:Showed a dose-dependent reduction in overall nociceptive behavior.
体外研究：
AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons.The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM.
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