Chemical Structure : VU0255035
CAS No.: 1135243-19-4
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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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.
M.Wt | 432.517 | |
Formula | C18H20N6O3S2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(3-oxo-3-(4-(pyridine-4-yl)piperazin-1-yl)propyl)-benzo[c][1,2,5]thiadiazole-4 sulfonamide |
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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