ML380

• Description :

  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].

• 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.

• 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 :

  MAChR1; mAChR3; mAChR5

• CAS Number :

  [1627138-52-6]