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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MAChR5
Available Sizes
Frequently Asked Questions
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