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。
货号:ajcx16858
CAS:1494581-70-2
分子式:C24H31FN2O4S
分子量：462.58
溶解度:DMSO: 125 mg/mL (270.22 mM)
纯度：98%
存储：Store at -20°C
库存：现货

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.