产品
编 号：F175089
分子式：C24H31FN2O4S
分子量：462.58
分子式：C24H31FN2O4S
分子量：462.58
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 1494581-70-2
产品详情
生物活性：
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
体内研究：
GDC-0276 (口服；0.5-5 mg/kg) 显示 14C 富集，观察到的比活度为 22.6 μCi/mg。尿液中未检测到 GDC-0276；然而，尿液中的代谢物观察到 14C 富集，观察到的比活性为 19.6 μCi/mg。Animal Model:Six drug-na?ve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)
Dosage:0.5, 1, 2, 3, 4, 5 mg/kg
Administration:Oral adminstration
Result:Showed mean specific activities of 12.2 μCi/mg (a 24% enrichment) (n=4 animals) and 23.5 μCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
体内研究：
GDC-0276 (口服；0.5-5 mg/kg) 显示 14C 富集，观察到的比活度为 22.6 μCi/mg。尿液中未检测到 GDC-0276；然而，尿液中的代谢物观察到 14C 富集，观察到的比活性为 19.6 μCi/mg。Animal Model:Six drug-na?ve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)
Dosage:0.5, 1, 2, 3, 4, 5 mg/kg
Administration:Oral adminstration
Result:Showed mean specific activities of 12.2 μCi/mg (a 24% enrichment) (n=4 animals) and 23.5 μCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.
产品资料
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