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DS-1971a

DS-1971a 是选择性、口服有效的 NaV1.7抑制剂，对 hNaV1.7 和 mNaV1.7 的 IC50分别为 22.8 和 59.4 nM。DS-1971a 在缓解疼痛方面有研究价值。

CAS号

1450595-86-4

分子式

C20H21ClFN5O3S

主要靶点

Sodium Channel

仅限科研使用

Cat No : CM06483

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Synonyms

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  • CAS No.: 1450595-86-4

    DS-1971a
    CAS#: 1450595-86-4

产品信息

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

CAS号 1450595-86-4
分子式 C20H21ClFN5O3S
主要靶点 Sodium Channel
主要通路 离子通道
分子量 465.93
纯度 ， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

hNaV1.7:22.8 nM|mNav1.7:59.4 nM

体内活性

DS-1971a (0.1-1 mg/kg; p.o.) shows mitigated thermal hyperalgesia in a dose-dependent manner in partial sciatic nerve ligation (PSL) mice with ED50 of 0.32 mg/kg[1].

体外活性

DS-1971a showed high NaV1.7 inhibitory potency in vitro. The IC50 values are of 22.8 nM for hNaV1.7 and 59.4 mM for mNaV1.7[1].

溶解度

DMSO:100 mg/mL (214.62 mM)

参考文献

1.Shinozuka T, et al. Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor [published online ahead of print, 2020 May 26]. J Med Chem. 2020;10.1021/acs.jmedchem.0c00259.

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