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VU0255035

Chemical Structure : VU0255035

CAS No.: 1135243-19-4

VU0255035 (ML012, VU 0255035)

Catalog No.: PC-60736Not For Human Use, Lab Use Only.

VU0255035 (ML012) is a potent, selective, CNS penetrant and competitive orthosteric antagonist of M1 mAChR with IC50 of 132 nM, >75-fold selectivity over M2-M5.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

VU0255035 (ML012) is a potent, selective, CNS penetrant and competitive orthosteric antagonist of M1 mAChR with IC50 of 132 nM, >75-fold selectivity over M2-M5.
VU0255035 inhibits potentiation of NMDA receptor currents by the muscarinic agonist carbachol in hippocampal pyramidal cells, antagonizes PI hydrolysis in rat hippocampal slices induced by the mAChR agonist CCh with IC50 of 2.4 uM.
VU0255035 inhibits pilocarpine-induced seizures and reduces pilocarpine-induced mortality in mice.

Physicochemical Properties

M.Wt 432.517
Formula C18H20N6O3S2
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

N-(3-oxo-3-(4-(pyridine-4-yl)piperazin-1-yl)propyl)-benzo[c][1,2,5]thiadiazole-4 sulfonamide

References

1. Sheffler DJ, et al. Mol Pharmacol. 2009 Aug;76(2):356-68.

2. Weaver CD, et al. Curr Top Med Chem. 2009;9(13):1217-26.

3. Xiang Z, et al. J Pharmacol Exp Ther. 2012 Mar;340(3):595-603.

4. Witkin JM, et al. J Pharmacol Exp Ther. 2014 Nov;351(2):448-56.

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