VU0364572 (trifluoroacetate salt) - CAS:1240514-89-9

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VU0364572 (trifluoroacetate salt) (Synonyms:VU0364572 TFA)

目录号 : KCM10787 CAS No. : 1240514-89-9 纯度 : ≥98%

Data Sheet 产品使用指南

VU0364572 is a potent and selective agonist of the muscarinic acetylcholine receptor 1 (M; EC = 0.2 mM compared to >10 mM for M-M). It induces concentration-dependent increases in Ca mobilization and ERK1/2 phosphorylation in CHO cells transfected with the human M receptor (ECs = 0.89 and 10 mM, respectively) with no effect on β-arrestin recruitment. VU0364572 also improves hippocampal-dependent spatial learning and localization abilities and acquistion of contextual fear learning but cannot reverse amphetamine-induced hyperlocomotion in rats. This suggests therapeutic potential of VU0364572 for the treatment of Alzheimer's disease but not psychosis.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

VU0364572 (trifluoroacetate salt) is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 (trifluoroacetate salt) has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 (trifluoroacetate salt) is CNS penetrant.

体外研究

VU0364572 (30 μM; 25 min) TFA promotes the phosphorylation of KCNQ2, NR1, and MARCKS in striatal/NAc slices.

Western Blot Analysis

Cell Line:	Striatal/NAc slices
Concentration:	30 μM
Incubation Time:	25 min
Result:	Significantly increased the phosphorylation of KCNQ2 at T217, NR1 at S890, and MARCKS at S152/156.

体内研究

VU0364572 TFA (10 mg/kg/day; oral; 4 months) demonstrated neuroprotective effects in 5XFAD transgenic Alzheimer's disease mice. The half-life of VU0364572 is 45 minutes.

Animal Model:	5XFAD transgenic Alzheimer’s mice
Dosage:	10 mg/kg/day
Administration:	In drinking water, from 2 months of age to 6 months
Result:	Preserved hippocampal memory. Significantly reduced levels of soluble and insoluble Aβ 40,42 in the cortex and hippocampus of these animals. Significantly decreased oligomeric (oAβ) levels in the cortex.

分子式

C23H32F3N3O5

分子量

487.51

CAS号

1240514-89-9

中文名称

(3R)-3-[(2-甲基苯甲酰)氨基]-[1,4'-联哌啶]-1'-羧酸乙酯 2,2,2-三氟乙酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 55 mg/mL (112.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0512 mL	10.2562 mL	20.5124 mL
5 mM	0.4102 mL	2.0512 mL	4.1025 mL
10 mM	0.2051 mL	1.0256 mL	2.0512 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.75 mg/mL (5.64 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.64 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.75 mg/mL (5.64 mM); Clear solution

此方案可获得 ≥ 2.75 mg/mL (5.64 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。