| Bioactivity | LP-922761 hydrate 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 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors[1]. | |||||||||
| Target | IC50: 4.8 nM (Adapter protein-2 associated kinase 1 (AAK1) in enzyme assays); 7.6 nM (AAK1 in cell assays); 24 nM (BMP-2-inducible protein kinase (BIKE)) | |||||||||
| In Vivo | 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]. | |||||||||
| Name | LP-922761 hydrate | |||||||||
| Formula | C21H26N6O3.1/4H2O | |||||||||
| Molar Mass | 414.98 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| 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. |
LP-922761 hydrate
CAS: F: C21H26N6O3.1/4H2O W: 414.98
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with I
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