For research use only. Not for therapeutic Use.
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors[1].
In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment[1].
| Catalog Number | I016657 |
| CAS Number | 1454808-95-7 |
| Synonyms | tert-butyl N-[2-[[3-(4-carbamoylphenyl)imidazo[1,2-b]pyridazin-6-yl]amino]ethyl]-N-methylcarbamate |
| Molecular Formula | C21H26N6O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H26N6O3/c1-21(2,3)30-20(29)26(4)12-11-23-17-9-10-18-24-13-16(27(18)25-17)14-5-7-15(8-6-14)19(22)28/h5-10,13H,11-12H2,1-4H3,(H2,22,28)(H,23,25) |
| InChIKey | YNQNYIHMAZLJAV-UHFFFAOYSA-N |
| SMILES | CC(C)(C)OC(=O)N(C)CCNC1=NN2C(=NC=C2C3=CC=C(C=C3)C(=O)N)C=C1 |
| Reference | [1]. Kostich W, et al. Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain. J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. |
