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首页-小分子抑制剂&激动剂-Others-AP2-associated Kinase 1 (AAK1)-LX9211
LX9211

Chemical Structure : LX9211

CAS No.: 1815613-42-3

LX9211 (BMS-986176, LX-9211, BMS986176)

货号: PC-72847Not For Human Use, Lab Use Only.

LX9211 (BMS-9861761) is a highly selective, CNS-penetrable, and potent AAK1 inhibitor with IC50 of 2.0 nM.

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5 mg ¥2480 In stock
10 mg ¥3980 In stock
25 mg ¥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LX9211 (BMS-9861761) is a highly selective, CNS-penetrable, and potent AAK1 inhibitor with IC50 of 2.0 nM.
BMS-986176 showed excellent efficacy in two rodent neuropathic pain models and excellent central nervous system (CNS) penetration and target engagement at the spinal cord with an average brain to plasma ratio of 20 in rat.
BMS-986176 exhibited favorable physicochemical and pharmacokinetic properties, had an acceptable preclinical toxicity profile
BMS-986176 has completed phase I trials with good human pharmacokinetics and minimum adverse events and is currently in phase II clinical trials for diabetic peripheral neuropathic pain.

物理化学性质&存储条件

分子量 385.407
分子式 C19H23F4N3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine

参考文献

1. Luo G, et al. J Med Chem. 2022 Mar 8. doi: 10.1021/acs.jmedchem.1c02131.

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