VU6000918

Names

[ CAS No. ]:
2101737-32-8

[ Name ]:
VU6000918

Biological Activity

[Description]:

VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

[Target]

EC50: 19 nM (hM4)[1].

[In Vitro]

VU6000918 demonstrates statistically significant AHL reversal (18%) from a low oral dose of 0.03 mg/kg and reaches maximal reversal (74%) from a 3 mg/kg dose, with a resulting in vivo plasma EC50 of 74 nM (0.66 nM unbound) based on terminal concentrations measured in the study animals (1.5 hr post-administration of 17j)[1].

[References]

[1]. James C Tarr, et al. Challenges in the development of an M 4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2990-2995.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₇F₂N₅OS

[ Molecular Weight ]:
389.42

Related Compounds

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