| Bioactivity | ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease[1]. |
| Target | EC50: 1.38 µM (M1 mAChR) |
| Invitro | ML169 (VU0405652) is selective versus the biogenic amines (D2, H-HT2B, etc...) and displays no orthosteric binding at M1–M5[1].ML169 shifts APP processing towards a non-amyloidogenic pathway[1].ML169 (2 µM) potentiates the carbachol (CCh)-mediated non-amyloidogenic APPsa release to the same degree as 10 µM CCh[1]. |
| In Vivo | ML169 (VU0405652) (10 mg/kg; i.p.) affords a brainAUC/plasmaAUC of 0.32 at 1 h in rats[1]. |
| Name | ML169 |
| CAS | 1222878-02-5 |
| Formula | C21H17BrFN3O4S |
| Molar Mass | 506.34 |
| 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]. Reid PR, et al. Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. Bioorg Med Chem Lett. 2011 May 1;21(9):2697-701. |