BMS-911172 is a potent and brain-penetrant, AP2-associated protein kinase 1 (AAK1)-selective inhibitor (IC50 = 12 and 51 nM in enzymes and cells, respectively). BMS-911172 was active in the formalin assay in the Chung mouse model (60 mg/kg s.c.) as well as in the chronic constriction injury-induced thermal hyperalgesia and mechanical allodynia rat model (60 mg/kg). PD marker assay in mice showed a dose-dependent inhibition of phosphorylation of AAK1 substrate mu-2 in the brain. There were no motor side effects at the doses tested. BMS-911172 may be useful for the treatment of neuropathic pain
MedKoo Cat#: 522617
Name: BMS-911172
CAS#: 1644248-18-9 (free base)
Chemical Formula: C16H19F2N3O3
Exact Mass: 339.1394
Molecular Weight: 339.34
Elemental Analysis: C, 56.63; H, 5.64; F, 11.20; N, 12.38; O, 14.14
The following data is based on the product molecular weight 339.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
