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LX9211

Chemical Structure : LX9211

CAS No.: 1815613-42-3

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

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 385.407
Formula C19H23F4N3O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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