VU0357017

VU0357017 (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM) . VU0357017 can be used for the research of Alzheimer’s disease and schizophrenia[1][2][3].

Product Specifications

CAS Number

[1135681-23-0]

Product Name Alternative

CID-25010775 (free base)

UNSPSC

12352005

Target

MAChR

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Smiles

O=C(N1CCC(NCCNC(C2=CC=CC=C2C)=O)CC1)OCC

Molecular Formula

C18H27N3O3

Molecular Weight

333.43

References & Citations

[1]Digby GJ, et al. Chemical modification of the M (1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. ACS Chem Neurosci. 2012 Dec 19;3 (12) :1025-36.|[2]Lebois EP, et al. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M (1) receptor function in the central nervous system. ACS Chem Neurosci. 2010;1 (2) :104-121.|[3]Digby GJ, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci. 2012 Jun 20;32 (25) :8532-44.|[4]Sheffler DJ, et al. Further exploration of M? allosteric agonists: subtle structural changes abolish M? allosteric agonism and result in pan-mAChR orthosteric antagonism. Bioorg Med Chem Lett. 2013 Jan 1;23 (1) :223-7.