GDC-0276

GDC-0276 是一种有效的、选择性的、可逆的口服活性 NaV1.7 抑制剂，其 IC50 值为 0.4 nM。GDC-0276 耐受性良好，显现良好的药代动力学特征。GDC-0276 有潜力用于治疗疼痛以及解决现有止痛药物缺陷，如成瘾和脱靶副作用的相关研究。

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库存: 现货

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价格

促销价

数量
5mg

￥4850.00

3880.00

- +
10mg

￥8412.00

6730.00

- +
50mg

￥25650.00

20520.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

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[1].

[1]. Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i [2]. Steven J. McKerrall, et al. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018) [3]. Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44.