|4-((2-(2-甲基苯甲酰氨基)乙基)氨基)哌啶-1-羧酸乙酯盐酸盐|CsnPharm

CAS No.: 1135242-13-5

VU0357017 HCl Catalog No. CSN15876

Synonyms: CID-25010775;VU0357017 (hydrochloride);VU-0357017

VU 0357017 HCl is a positive allosteric modulator of muscarinic M1 receptors with EC50 value of 198 nM.

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技术信息

生物活性

描述VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15). Ki values of VU0357017 derived from competition binding experiment is 9.91(rM1), 21.4 (rM2), 55.3 (rM3), 35 (rM4), and 50 (rM5), respectively^[1]. VU0357017 has robust effects on M1-activation of calcium mobilization and ERK1/2 phosphorylation but have little effect on β-arrestin recruitment. VU0357017 induces calcium release and ERK phosphorylation but is without effects on β-arrestin recruitment. VU0357017 significantly enhances threshold theta-burst LTP and VU0364572 induces LTD at the Schaffer collateral-CA1 synapse of rodent hippocampal slices. VU0357017 has robust efficacy in improving hippocampal-dependent learning in rats. VU0357017 enhances performance in Morris water maze and contextual fear conditioning in rats^[3].
参考文献

[1] Digby GJ, Utley TJ, Lamsal A, et al. Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode. ACS Chem Neurosci. 2012;3(12):1025-1036
[2] Lebois EP, Bridges TM, et al. Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system. ACS Chem Neurosci. 2010;1(2):104-121.
[3] Digby GJ, Noetzel MJ, Bubser M, et al. Novel allosteric agonists of M1 muscarinic acetylcholine receptors induce brain region-specific responses that correspond with behavioral effects in animal models. J Neurosci. 2012;32(25):8532-8544

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7035 mL
- 13.5177 mL
- 27.0353 mL
- 5 mM
- 0.5407 mL
- 2.7035 mL
- 5.4071 mL
- 10 mM
- 0.2704 mL
- 1.3518 mL
- 2.7035 mL

技术信息

CAS号

1135242-13-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H28ClN3O3

运输

蓝冰

分子量

369.89

别名

CID-25010775;VU0357017 (hydrochloride);VU-0357017

溶解度

DMSO	78.0 mg/mL (210.9 mM) warming
Water	insoluble

动物实验配方

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