货号	规格	价格	上海	北京	珠海	重庆	武汉
S89689-5mg买3赠1	99.60%	￥400.00 S89689-5mg ￥400.00 现货（买3赠1）	7 7	-	-	-	-
S89689-10mg买3赠1	99.60%	￥750.00 S89689-10mg ￥750.00 现货（买3赠1）	8 8	-	-	-	-
S89689-25mg促销	99.60%	￥1300.00 ￥1040.00 S89689-25mg ￥1040.00 现货	6 6	-	-	-	-
S89689-100mg促销	99.60%	￥3750.00 ￥3000.00 S89689-100mg ￥3000.00 现货	2 2	-	-	-	-

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产品描述：

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

靶点：

Autophagy

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.

体内研究：

CA77.1 (oral gavage; 10 mg/kg;single dose) demonstrates brain penetrance with favorable pharmacokinetics. The Cmax, AUClast, Tmax and T1/2 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. 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.

参考文献：

1. Mathieu Bourdenx, et al. Chaperone-mediated autophagy prevents collapse of the neuronal metastable proteome.Cell. 2021 May 13;184(10):2696-2714.e25.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

2-8℃，避光保存

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.359 ml	16.793 ml	33.586 ml
5 mM	0.672 ml	3.359 ml	6.717 ml
10 mM	0.336 ml	1.679 ml	3.359 ml
50 mM	0.067 ml	0.336 ml	0.672 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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