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LY 379268

目录号: PC14577 纯度: ≥98%
II组mGlu受体激动剂,Highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors.
CAS No. :191471-52-0
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Medlife所售产品仅用于科学研究(非临床研究),非药品不可食用,不可用于人体或动物的临床诊断和治疗,我们不为个人提供产品及服务。产品COA等资料,可至下方“质量控制”中下载。
中文名称
LY 379268
英文名称
LY 379268
英文别名
LY 379268;(1R,4R,5S,6R)-4-amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylic acid;CHEBI:104347;CHEMBL275079;CTK8F0567;DNC007065;LS-98795;LY-379268;SureCN2454646;LY397268;(1R,4R,5S,6R)-4-Amino-2-oxabicyclo[3.1.0]hexane-4,6-dicarboxylicacid;2-Oxabicyclo[3.1.0]hexane-4,6-dicarboxylicacid,4-amino-,(1R,4R,5S,6R)-
Cas No.
191471-52-0
分子式
C7H9NO5
分子量
187.15
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

LY379268 is a potent, selective and brain-penetrant mGlu2/3R agonist with EC50 values of 2.69 nM (mGlu2) and 4.48 nM (mGlu3). LY379268 has no activity on human mGlu 1a, 4a, 5a or 7a receptors. LY379268 has antioxidant and neuroprotective effects.

性状

Solid

IC50 & Target[1][2]

hmGluR2

2.69 nM (EC50)

hmGluR3

4.48 nM (EC50)

hmGluR2

14.1 nM (Ki)

hmGluR3

5.8 nM (Ki)

体外研究(In Vitro)

Treatment of 9-weeks (9w) astrocytes with LY379268 (0.1 μM; 24-48 hours) results in an increase in mGlu3R and Nrf2 protein levels and SOD activity, and decreases mitochondrial ROS levels and apoptosis. mGlu3R activation in aged astrocytes also preventS hippocampal neuronal death induced by Aβ1-42 in co-culture assays. Activation of mGlu3R in aged astrocytes haS an anti-oxidant effect and protected hippocampal neurons against Aβ-induced neurotoxicity.

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

体内研究(In Vivo)

For LY379268, when a 3?mg/kg dose is given prior to an intraplantar injection of carrageenan, the inflammatory hyperalgesia that developed is significantly delayed, without affecting the inflammation of the paw.
In a model of mouse tail withdrawal to warm water, LY379268 (12?mg/kg; i.p.), given before a subcutaneous tail injection of capsaicin, reduces the subsequent neurogenic hyperalgesia.

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

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

0.1 M NaOH : 200 mg/mL (1068.66 mM; ultrasonic and adjust pH to 8 with NaOH)

H2O : 2 mg/mL (10.69 mM; ultrasonic and adjust pH to 10 with NaOH)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.3433 mL 26.7165 mL 53.4331 mL
5 mM 1.0687 mL 5.3433 mL 10.6866 mL
10 mM 0.5343 mL 2.6717 mL 5.3433 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: PBS

    Solubility: 25 mg/mL (133.58 mM); Clear solution; Need ultrasonic

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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