AA147|cas:393121-74-9|西域试剂

AA147,99.89%

产品编号：Bellancom-124293| CAS NO：393121-74-9| 分子式：C₁₆H₁₇NO₂| 分子量：255.31

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货号	价格	库存与货期
Bellancom-124293	￥600.00	杭州北京（现货）
Bellancom-124293	￥950.00	杭州北京（现货）
Bellancom-124293	￥1800.00	杭州北京（现货）
Bellancom-124293	￥2880.00	杭州北京（现货）
Bellancom-124293	￥4600.00	杭州北京（现货）

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AA147

产品介绍

AA147 是一种内质网 (ER) 蛋白稳态调节剂。AA147 可通过选择性激活未折叠蛋白反应的 ATF6 臂以及激活 NRF2 氧化应激反应来促进对神经元细胞氧化损伤的保护，并防止内皮屏障功能失调。AA147 还可重新平衡 XBP1s 在体内的表达，并诱导运动神经元存活基因的表达并保护脊柱运动神经元。

生物活性

AA147 is a endoplasmic reticulum (ER) proteostasis regulator. AA147 promotes protection against oxidative damage in neuronal cells and prevents endothelial barrier dysfunction by activating ATF6 arm (selectively) of the unfolded protein response (UPR) and the NRF2 oxidative stress response. AA147 can rebalances XBP1s expression in vivo, and also induces survival motor neuron (SMN) expression and spinal motorneuron (MN) protection^[4].

体外研究

AA147 (20-0.078 μM (dilution in half); 6 or 16 h) protects against glutamate-induced oxidative toxicity in HT22 cells by decreasing the reactive oxygen species (ROS)-associated damage.
AA147 (10 μM; 16 h) induces NRF2-dependent upregulation of oxidative stress response genes in HT22 cells.
AA147 (10 μM; 16 h) covalently modifies KEAP1 to promote NRF2 activation in HT22 cells.
AA147 (5, 10, 15 μM; 4, 8, 16, 24, 48 h) induces ATF6 activation and upregulates phosphorylation of cofilin in BPAEC.
AA147 (10 μM; 24 h) reduces LPS-induced endothelial barrier disruption in BPAEC.
AA147 (5, 10 μM; 135 h) enhances lung endothelial barrier integrity.

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

Cell Viability Assay

Cell Line:	HT22 cells
Concentration:	0.078, 0.156, 0.312, 0.625, 1.25, 2.5, 5, 10, 20 μM
Incubation Time:	6 or 16 h (pre-incubation)
Result:	Showed dose-dependent increases in the viability of glutamate-treated HT22 cells when pretreated with AA147 for 6 or 16 h prior to the glutamate challenge (addition concurrently with the glutamate challenge did not improve the viability of glutamate-treated cells). Reduced ROS accumulation in cells when pre-incubation of 16 h.

Cell Viability Assay

Cell Line:	HT22 cells
Concentration:	10 μM
Incubation Time:	16 h
Result:	Significant increased the expression of genes associated with antioxidant activity in neuronal models, including prolactins and glutathione transferases. Activated NRF2 through a mechanism involving metabolic activation and covalent KEAP1 protein modification.

Cell Viability Assay

Cell Line:	BPAEC
Concentration:	5, 10 μM
Incubation Time:	135 h
Result:	Decreased permeability of cells by activation of ATF6.

Western Blot Analysis

Cell Line:	BPAEC
Concentration:	5, 10, 15 μM
Incubation Time:	4, 8, 16, 24, 48 h
Result:	Significantly induced ATF6 activation and upregulated cofilin phosphorylation (in a concentration-dependent manner).

Western Blot Analysis

Cell Line:	BPAEC
Concentration:	10 μM
Incubation Time:	24 h
Result:	Reduced LPS-induced cATF6 suppression (Fig.5A) and VE-cadherin phosphorylation. Inhibited cofilin and MLC2 activation in the inflamed cells. Inhibited LPS-induced hyperpermeability in BPAEC.

体内研究
(In Vivo)

AA147 (intrathecal injection; single for 3 days) can rebalance XBP1s expression in severe SMA-like mice by activating ATF6, and also induce survival motor neuron expression and spinal motorneuron protection.

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

体内研究

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (195.84 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.9168 mL	19.5840 mL	39.1681 mL
5 mM	0.7834 mL	3.9168 mL	7.8336 mL
10 mM	0.3917 mL	1.9584 mL	3.9168 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (19.58 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (19.58 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 5 mg/mL (19.58 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (19.58 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 50.0 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