VU0255035 (ML012) | M1 mAChR antagonist | Probechem Biochemicals

Chemical Structure : VU0255035

CAS No.: 1135243-19-4

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VU0255035 (ML012, VU 0255035)

货号: 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.

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1580	In stock
25 mg	￥2780	In stock
50 mg	￥4880	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	432.517
分子式	C18H20N6O3S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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

参考文献

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.

VU0255035 (ML012, VU 0255035)

生物&药学活性

物理化学性质&存储条件

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VU0255035 (ML012, VU 0255035)

生物&药学活性

物理化学性质&存储条件

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