VU0255035

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Chemical Structure| 1135243-19-4 同义名 : -
CAS号 : 1135243-19-4
货号 : A723827
分子式 : C18H20N6O3S2
纯度 : 95%
分子量 : 432.52
MDL号 : -
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 VU0255035, a potent (IC50 = 130 nM) and selective small molecule M(1) antagonist. VU0255035 was centrally penetrant (Brain(AUC)/Plasma(AUC) of 0.48) and active in vivo, rendering it acceptable as both an in vitro and in vivo MLSCN/ MLPCN probe molecule for studying and dissecting M(1) function[2]. VU0255035 significantly suppressed seizure severity and prevented the development of SE (status epilepticus) for about 40 minutes after exposure to paraoxon or soman, suggesting an important role of the M1 receptor in the early phases of seizure generation[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL
参考文献

[1]Sheffler DJ, Williams R, et al. A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol Pharmacol. 2009 Aug;76(2):356-68.

[2]Weaver CD, Sheffler DJ, Lewis LM, Bridges TM, Williams R, Nalywajko NT, Kennedy JP, Mulder MM, Jadhav S, Aldrich LA, Jones CK, Marlo JE, Niswender CM, Mock MM, Zheng F, Conn PJ, Lindsley CW. Discovery and development of a potent and highly selective small molecule muscarinic acetylcholine receptor subtype I (mAChR 1 or M1) antagonist in vitro and in vivo probe. Curr Top Med Chem. 2009;9(13):1217-26.

[3]Miller SL, Aroniadou-Anderjaska V, Pidoplichko VI, Figueiredo TH, Apland JP, Krishnan JK, Braga MF. The M1 Muscarinic Receptor Antagonist VU0255035 Delays the Development of Status Epilepticus after Organophosphate Exposure and Prevents Hyperexcitability in the Basolateral Amygdala. J Pharmacol Exp Ther. 2017 Jan;360(1):23-32.