LY379268

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LY379268

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

191471-52-0

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议

产品介绍

LY379268 是一种有效、选择性和可透过血脑屏障的mGlu2/3R激动剂，EC₅₀值为 2.69 nM (mGlu2) 和 4.48 nM (mGlu3)。LY379268 对人 mGlu 1a、4a、5a 或 7a 受体没有活性。LY379268 具有抗氧化和神经保护作用。

生物活性

LY379268 is a potent, selective and brain-penetrantmGlu2/3Ragonist withEC₅₀values 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^[1]^[2].

IC₅₀& Target^[1]

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^[3].

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^[2].
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^[2]. LY354740 prevents release of glutamate in the striatum in freely moving rats and to attenuate morphine withdrawal-associated activation of locus coeruleus neurones, thought to be caused by an increased release of glutamate^[2].

分子量

187.15

性状

Solid

Formula

C₇H₉NO₅

CAS 号

191471-52-0

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	6 months
	-20°C	1 month

溶解性数据

In Vitro:

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

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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： PBS
Solubility: 25 mg/mL (133.58 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。