| Bioactivity | ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies[1][2]. |
| Target | IC50: 450 nM (mAChR M5). |
| In Vivo | ML381 (0.2 mg/kg; i.v.; single) 在大鼠药效学研究中具有总体可接受的 DMPK 特征，但代谢稳定性差，且在血浆中可能发生酰胺水解；因此最适合作为体外/电生理探针使用[1]。 Animal Model: |
| Name | ML381 |
| CAS | 1623481-80-0 |
| Formula | C21H21N3O4 |
| Molar Mass | 379.41 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gentry PR, et al. Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe. ChemMedChem. 2014 Aug;9(8):1677-82. |