CA77.1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CA77.1(CA) 是一种新型伴侣介导的自噬 (CMA) 激活剂，用于治疗阿尔茨海默病 (AD)。

CA77.1(CA) is a novel chaperon-mediated autophagy (CMA) activator for the treatment of Alzheimer's disease (AD).

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.

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.

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Autophagy

Autophagy

autophagy

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2412270-22-3

297.74

C16H12ClN3O

>98% (HPLC)

DMSO:10 mM

CC(NC1=CC=C(C2=NC3=CC=C(Cl)C=C3N=C2)C=C1)=O

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(-20℃)

With Ice Pack

≥ 2 years