ML381 fumarate | M5 mAChR antagonist | Probechem Biochemicals

Chemical Structure : ML381 fumarate

ML381 fumarate (VU0488130 fumarate)

Catalog No.: PC-62144Not For Human Use, Lab Use Only.

ML381 (VU0488130) is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).

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Biological Activity

ML381 (VU0488130) fumarate is a highly mAChR subtype selective M5 orthosteric antagonist with IC50/Ki of 450/340 nM for hM5, has no inhibitory activity on hM1-4 (IC50>30 uM).
ML381 exhibits good DMPK properties and CNS penetration (B:P ratio of 0.58) to support both in vitro and in vivo studies.

Physicochemical Properties

M.Wt	495.488
Formula	C25H25N3O8
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-[(3-Acetylphenoxy)methyl]-N-methyl-N-[(1S)-1-pyridin-2-ylethyl]-1,2-oxazole-3-carboxamide fumarate

References

1. Gentry PR, et al. ChemMedChem. 2014 Aug;9(8):1677-82.

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ML381 fumarate (VU0488130 fumarate)

Biological Activity

Physicochemical Properties

References

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