CA77.1|cas:2412270-22-3|西域试剂

CA77.1,99.45%

产品编号：Bellancom-134923| CAS NO：2412270-22-3| 分子式：C₁₆H₁₂ClN₃O| 分子量：297.74

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-134923	￥600.00	杭州北京（现货）
Bellancom-134923	￥1000.00	杭州北京（现货）
Bellancom-134923	￥2000.00	杭州北京（现货）
Bellancom-134923	￥3200.00	杭州北京（现货）
Bellancom-134923	￥5000.00	杭州北京（现货）

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CA77.1

产品介绍

CA77.1 是一种有效的，具有脑渗透性和口服活性的分子伴侣介导自噬 (CMA) 的激活剂，表现出良好的药代动力学。CA77.1是 AR7 的衍生物，可以增加溶酶体受体 (LAMP2A) 在溶酶体中的表达。CA77.1 可以改善 PS19 小鼠模型的行为和神经病理特征，可用于阿尔茨海默病的研究。

生物活性

CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research.

体外研究

CA77.1 (0-30 μM; 16 hours) activates CMA in a dose-and time-dependent manner to NIH 3T3 cells stably expressing the KFERQ-PS-Dendra reporter. The CMA activity is quantified as the average of fluorescent puncta per cell.
CA77.1 (20 μM; 6 hours) does not alter on LC3-II expression, and does not effects autophagic flux in NIH 3T3 cells.

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

体内研究

CA77.1 (oral gavage; 10 mg/kg;single dose) demonstrates brain penetrance with favorable pharmacokinetics. The C_max, AUC_last, T_max and T_1/2 are 3534 ng/g, 8338 h*ng/g, 1 hour and 1.89 hour, respectively.
CA77.1 (oral gavage; 30 mg/kg; 6 months) normalizes the previously described locomotor hyperactivity of PS19 mice to control levels. And it reduces the levels and number of neurons containing pathogenic tau conformations in the hippocampus, amygdala, and piriform cortex. And the higher number of microglial cells and presence of large Iba1-positive cells with rod-like dystrophic morphology in vehicle-treated PS19 mice are reduced upon CA77.1 treatment.

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

Animal Model:	9-month-old CTR or PS19 mice
Dosage:	30 mg/kg
Administration:	Oral gavage; 30 mg/kg; 6 months
Result:	Improved behavior and neuropathology in a mouse model of frontotemporal-dementia-related proteotoxicity.

体内研究

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

Animal Model:	9-month-old CTR or PS19 mice
Dosage:	30 mg/kg
Administration:	Oral gavage; 30 mg/kg; 6 months
Result:	Improved behavior and neuropathology in a mouse model of frontotemporal-dementia-related proteotoxicity.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (16.79 mM; ultrasonic and warming and heat to 60°C)

Ethanol : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3586 mL	16.7932 mL	33.5864 mL
5 mM	0.6717 mL	3.3586 mL	6.7173 mL
10 mM	0.3359 mL	1.6793 mL	3.3586 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 (protect from light)。-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