AZ 12216052 - CAS:1290628-31-7

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AZ 12216052

目录号 : KCM10939 CAS No. : 1290628-31-7 纯度 : ≥98%

Data Sheet SDS 产品使用指南

AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8). It potentiates glutamate-induced [S]GTPγS binding in GHEK cells expressing human mGluR8b (EC = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM. AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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.

体外研究

AZ 12216052 (10 μM) enhances the peak excitation current of ON - and OFF - currents in ON-OFF ganglion cells, depending on the intensity of light stimulation [1].
AZ 12216052 showed an effect on cell differentiation and (0.01-1 μM; 24-48 hours) reduced Dox induced partial damage to human neuroblastoma SH-SY5Y cells [2].
AZ 12216052 stimulates proliferation and attenuates toxicity induced by erythromycin (St) and doxorubicin (Dox) in UN-SH-SY5Y cells [2].
AZ12216052 (10 μM) enhances the glutamate activity of human mGluR8b receptor expressed in GHEK cells [3].

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

AZ 12216052 (10 mg/kg; intraperitoneal injection; Reduce anxiety 2 hours before testing without affecting the speed of mice.
AZ12216052 (10 mg/kg; intraperitoneal injection; Single dose) showed anti anxiety effects, possibly involving mGluR4 in mGluR8/mice, as mGluR4 PAM (positive allosteric modulator) VU 0155041 can also reduce anxiety levels in wild-type mice.

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.

分子式

C₁₉H₂₂BrNOs

分子量

392.35412

CAS号

1290628-31-7

中文名称

AZ 12216052

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:

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	5.8933 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。
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。