VU0483605 - CAS:1623101-11-0

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VU0483605

目录号 : KCM11814 CAS No. : 1623101-11-0 纯度 : ≥98%

Data Sheet 产品使用指南

Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation. VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1, displaying EC values of 0.39 and 0.36 μM at human and rat receptors, respectively, and no activity as a mGlu4 PAM (EC >10 μM). It has been shown to potentiate a response to glutamate in wild-type cell lines stably expressing mGlu1 and to partially restore the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively[1].

体外研究

VU0483605 proves superior with excellent mGlu1 PAM activity at both human (EC50 = 390 nM) and rat (EC50 = 356 nM, pEC50 = 6.45 ± 0.11, 113 ± 5% Glu Max) and no activity as an mGlu4 PAM (EC50 >10 μM)[1].

分子式

C₂₀H₁₀Cl₃N₃O₃

分子量

446.7

CAS号

1623101-11-0

中文名称

VU0483605

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : 100 mg/mL (223.88 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2388 mL	11.1939 mL	22.3879 mL
5 mM	0.4478 mL	2.2388 mL	4.4776 mL
10 mM	0.2239 mL	1.1194 mL	2.2388 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 (protect from 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: ≥ 2.5 mg/mL (5.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 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。