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ML380 

Cat. No. M28716

All AbMole products are for research use only, cannot be used for human consumption.

ML380  Structure
Size Price Availability Quantity
5mg USD 85 In stock
10mg USD 145 In stock
25mg USD 245 In stock
50mg USD 450 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 494.53
Formula C23H25F3N4O3S
CAS Number 1627138-52-6
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Alice E Berizzi, et al. ACS Chem Neurosci. Structure-Activity Relationships of Pan-Gαq/11 Coupled Muscarinic Acetylcholine Receptor Positive Allosteric Modulators

[2] Aaron M Bender, et al. ACS Chem Neurosci. Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold

[3] Alice E Berizzi, et al. Mol Pharmacol. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators

[4] Patrick R. Gentry, et al. Development of the First CNS penetrant M5 Positive Allosteric Modulator (PAM) Based on a Novel, non-Isatin Core

[5] Patrick R Gentry, et al. J Med Chem. 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)

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Keywords: ML380  supplier, AChR/AChE, inhibitors, activators

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