ML169

Names

[ Name ]:
ML169

[Synonym ]:
ml169

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

[Target]

EC50: 1.38 µM (M1 mAChR)[1]

[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₁₇BrFN₃O₄S

[ Molecular Weight ]:
506.34

[ Exact Mass ]:
505.01100

[ PSA ]:
102.58000

[ LogP ]:
5.45380

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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