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 amGluR8positive allosteric modulator, and helpsmGluR8modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect[1][2][3][4]. |
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体外研究
(In Vitro) | mGluR8 may modulates the synaptic inputs to retinal ganglion cells[1].
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[1].
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[2].
AZ 12216052 stimulates proliferation and attenuates staurosporine (St)- and doxorubicin (Dox)-induced toxicity in UN-SH-SY5Y cells[2].
AZ12216052 (10 μM) enhances glutamate activity of human mGluR8b receptor expressed in GHEK cells[3].
Cell Viability Assay[2] | 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. |
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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[3].
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].
| Animal Model: | WT and Apolipoprotein E-deficient (Apoe–/–) mice (C57BL/6J, 2-month-old) in the elevated zero maze[3] | | 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(254.87 mM;Need ultrasonic) 配制储备液 | 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℃, 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： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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。
*以上所有助溶剂都可在本网站选购。 |
