ML375

ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4[1].

Product Specifications

CAS Number

[1488362-55-5]

Product Name Alternative

VU0483253

UNSPSC

12352005

Target

MAChR

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ml375.html

Purity

99.70

Solubility

DMSO : 40 mg/mL (ultrasonic; warming)

Smiles

O=C1N2[C@@](N(C(C3=CC=C(F)C(F)=C3)=O)CC2)(C4=CC=C(Cl)C=C4)C5=C1C=CC=C5

Molecular Formula

C23H15ClF2N2O2

Molecular Weight

424.83

References & Citations

[1]Patrick R Gentry, et al. Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S) -9b- (4-chlorophenyl) -1- (3,4-difluorobenzoyl) -2,3-dihydro-1H-imidazo[2,1-a]isoindol-5 (9bH) -one (ML375) . J Med Chem. 2013 Nov 27;56 (22) :9351-5.|[2]Barak W Gunter, et al. Selective inhibition of M 5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats. Addict Biol. 2018 Sep;23 (5) :1106-1116.