ML380

ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR[1][2][3].

Product Specifications

CAS Number

[1627138-52-6]

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/ml380.html

Concentration

10mM

Purity

99.87

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1CCN(S(=O)(C2=CC3=C(NN=C3)C=C2)=O)CC1)N(CC)CC4=CC=CC=C4C(F)(F)F

Molecular Formula

C23H25F3N4O3S

Molecular Weight

494.53

References & Citations

[1]Gentry PR, et, al. Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1- ((1H-indazol-5-yl) sulfoneyl) -N-ethyl-N- (2- (trifluoromethyl) benzyl) piperidine-4-carboxamide (ML380) . J Med Chem. 2014 Sep 25;57 (18) :7804-10.|[2]Berizzi AE, et, al. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Mol Pharmacol. 2016 Oct;90 (4) :427-36.|[3]Berizzi AE, et, al. Structure-Activity Relationships of Pan-Gα q/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators. ACS Chem Neurosci. 2018 Jul 18;9 (7) :1818-1828.