AZ 12216052|cas:1290628-31-7|西域试剂

AZ 12216052,98.0%

产品编号：Bellancom-110122| CAS NO：1290628-31-7| 分子式：C₁₉H₂₂BrNOS| 分子量：392.35

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-110122		￥2360.00	杭州北京（现货）
Bellancom-110122		￥3776.00	杭州北京（现货）

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AZ 12216052

产品介绍

AZ 12216052 是一种 mGluR8 正变结构调节剂，帮助 mGluR8 调节视网膜神经节细胞的信号输入。AZ 12216052 具有抗焦虑作用。

生物活性

AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect^[4].

体外研究

mGluR8 may modulates the synaptic inputs to retinal ganglion cells.
AZ 12216052 (10 μM) enhances the peak excitatory currents of ON-, OFF- currents in ON-OFF-ganglion cells, with a dependent way on the intensity of the light stimuli.
AZ 12216052 shows impact of cell differentiation and (0.01-1 μM; 24-48 h) reduces Dox-induced human neuroblastoma SH-SY5Y cell damage partially.
AZ 12216052 stimulates proliferation and attenuates staurosporine (St)- and doxorubicin (Dox)-induced toxicity in UN-SH-SY5Y cells.
AZ12216052 (10 μM) enhances glutamate activity of human mGluR8b receptor expressed in GHEK cells.

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

Cell Viability Assay

Cell Line:	UN- and RA-SH-SY5Y cells
Concentration:	0.01-1 μM
Incubation Time:	48 hours
Result:	Increased cell viability at 0.1 μM, and protected undifferentiated neuroblastoma cells against damaging effects of Iri or Cis.

体内研究
(In Vivo)

AZ 12216052 (10 mg/kg; i.p.; 2 h prior to testing) reduces measures of anxiety, without affecting the velocity of the mice.
AZ12216052 (10 mg/kg; i.p.; single dose) exhibits remaining anxiolytic effects, might involve mGluR4 in mGluR8−/− mice, as the mGluR4 PAM (Positive Allosteric Modulator) VU 0155041 also reduces measures of anxiety in wild-type mice^[4].

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

Animal Model:	WT and Apolipoprotein E-deficient (Apoe−/−) mice (C57BL/6J, 2-month-old) in the elevated zero maze
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; singel dose, 2 h prior to testing
Result:	Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice. Reduced the acoustic startle response.

体内研究

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

Animal Model:	WT and Apolipoprotein E-deficient (Apoe−/−) mice (C57BL/6J, 2-month-old) in the elevated zero maze
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; singel dose, 2 h prior to testing
Result:	Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice. Reduced the acoustic startle response.

体内研究

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

Animal Model:	WT and Apolipoprotein E-deficient (Apoe−/−) mice (C57BL/6J, 2-month-old) in the elevated zero maze
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; singel dose, 2 h prior to testing
Result:	Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice. Reduced the acoustic startle response.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (254.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5487 mL	12.7437 mL	25.4874 mL
5 mM	0.5097 mL	2.5487 mL	5.0975 mL
10 mM	0.2549 mL	1.2744 mL	2.5487 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。-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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.37 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 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。