1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. Eglumegad

Eglumegad  (Synonyms: LY354740; Eglumetad)

目录号: HY-18941 纯度: 99.88%
COA 产品使用指南

Eglumegad (LY354740) 是一种有效,选择性的 group II (mGlu2/3) receptor 激动剂,对人 mGlu2mGlu3 受体的 IC50 分别为 5 nM 和 24 nM。

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Eglumegad Chemical Structure

Eglumegad Chemical Structure

CAS No. : 176199-48-7

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥1650
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5 mg ¥1500
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10 mg ¥2500
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25 mg ¥5000
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC50s of 5 nM and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.

IC50 & Target[1]

mGluR2R

5 nM (IC50)

mGluR3R

24 nM (IC50)

体外研究
(In Vitro)

Eglumegad (LY354740) 下调点 1014、1822 (缺氧上调蛋白 1)、4513 (蛋白质二硫化物异构酶 3 的同种型)、6204、6312、7306 (26S 蛋白酶体非 ATP 酶调节亚基 7) 和蛋白点 1013和 6005 (destrin),并上调小鼠皮层神经元中的斑点 6507 (塌陷蛋白反应介质蛋白 1)[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Eglumegad (LY354740) (15 或 30 mg/kg,腹腔注射) 对 Gria1 / 或 WT 小鼠的空间工作记忆性能没有影响,并且对短时间的奖励交替测试没有影响浓度为 30 mg/kg 的 Gria1 / 和 WT 小鼠的试验间隔。Eglumegad (LY354740) (15 或 30 mg/kg,腹腔注射) 降低野生型和 Gria1 / 小鼠[1]的自发运动活动。Eglumegad (LY354740) (15 mg/kg,ip) 在幼稚的 GluA1-KO 和预先处理过的 GluA1-KO 雄性中抑制新奇诱导的过度运动,但在雌性中则不然。Eglumegad (LY354740) (15 mg/kg,腹腔注射) 显著降低 GluA1-KO 雄性增加的 c-Fos 表达至 WT 雄性的水平,但对雌性没有影响[3]。Eglumegad (LY354740) (10 mg/kg,腹腔注射) 减弱大鼠 mPFC[4]中固定应激诱导的 BDNF mRNA 表达增加。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

185.18

Formula

C8H11NO4

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 33.33 mg/mL (179.99 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 6.33 mg/mL (34.18 mM; 超声加热助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.4002 mL 27.0008 mL 54.0015 mL
5 mM 1.0800 mL 5.4002 mL 10.8003 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (13.50 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 2.86 mg/mL (15.44 mM); 澄清溶液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.88%

参考文献
Animal Administration
[1][4]

Mice[1]
In Experiment 1A wild-type (female: N=6; male: N=5) and Gria1−/− mice (female: N=7; male: N=8) first receive 30 trials of drug-free testing (five trials per day for 6 days). Each animal is then tested on rewarded alternation following an injection of either Eglumegad (LY354740) (15 mg/kg) or vehicle. After injection animals are returned to the home cage for 30 min before behavioural testing commenced. Each animal is given 10 trials of rewarded alternation in the T-maze. Mice are given a maximum of 120 s to a complete a trial. At least 24 h after the first round of drug testing the animals are re-tested in the absence of any drug treatment to ensure that there are no long-term effects of the drug, and that the mice maintain a high level of alternation performance. Twenty-four hours after this re-testing, mice receive a further 10 trials of rewarded alternation testing, but now under the drug condition that they have not previously received. The order of drug exposure is counterbalanced within genotype and sex as far as possible given the numbers of mice. In all stages, the number of trials in which the animal alternated, as well as time taken to run from the start arm to the food well on the sample run (sample latency), and the time taken to run from the start arm to making a choice on the choice run (choice latency), are recorded. Latencies are measured by the experimenter using a stopwatch. The experimenter is blind to the genotype and drug allocations of the animals throughout testing. In Experiment 1B, separate groups of male wild-type (N=7) and Gria1−/− mice (N=7) undgo the same procedure as Experiment 1A but now they receive either vehicle or a higher dose of Eglumegad (LY354740) (30 mg/kg). Subsequently, in Experiment 1C, to investigate the potential effects of increased proactive interference, the procedure used in Experiment 1B is repeated in the same mice, using the same drug dose (30 mg/kg), but now using a modified testing protocol in which the interval between trials is reduced to 20 s.
Rats[4]
Two experiments are conducted. The first experiment compares the effects of LY354740 (10 mg/kg, i.p., neutralized to a pH ~ 7.4) or vehicle (0.9% saline neutralized to pH ~ 7.4) in rats remaining in their home cages or rats exposed to 2 h of immobilization stress in plastic cones (n=7, cage control/vehicle; n=7, cage control/LY354740; n=6, stress/vehicle; n=6, stress/Eglumegad (LY354740)). The second experiment compares two lower LY354740 doses (1 and 3 mg/kg, i.p.) or vehicle in rats exposed to a 2-h period of immobilization stress to rats treated with vehicle in their home cages (n=4 for all groups). All animals are injected with either Eglumegad (LY354740) or vehicle 15 min prior to being placed in plastic cones with the open end securely closed. All immobilized rats are placed in plexiglass chamber with animal bedding on the bottom; brought to a quiet room outside of the animal colony; and immediately placed in a plastic cone. Two hours after being placed in the plastic containers, the rats are decapitated. The brains are removed and frozen on dry ice, and stored at −80°C.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

Eglumegad 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 5.4002 mL 27.0008 mL 54.0015 mL 135.0038 mL
5 mM 1.0800 mL 5.4002 mL 10.8003 mL 27.0008 mL
10 mM 0.5400 mL 2.7001 mL 5.4002 mL 13.5004 mL
15 mM 0.3600 mL 1.8001 mL 3.6001 mL 9.0003 mL
20 mM 0.2700 mL 1.3500 mL 2.7001 mL 6.7502 mL
25 mM 0.2160 mL 1.0800 mL 2.1601 mL 5.4002 mL
30 mM 0.1800 mL 0.9000 mL 1.8001 mL 4.5001 mL
DMSO 40 mM 0.1350 mL 0.6750 mL 1.3500 mL 3.3751 mL
50 mM 0.1080 mL 0.5400 mL 1.0800 mL 2.7001 mL
60 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2501 mL
80 mM 0.0675 mL 0.3375 mL 0.6750 mL 1.6875 mL
100 mM 0.0540 mL 0.2700 mL 0.5400 mL 1.3500 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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