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ML380

CAT: 0804-HY-12439-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-12439-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
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

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