1. Autophagy
  2. Autophagy
  3. CA77.1

CA77.1 

Cat. No.: HY-134923
Handling Instructions

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.

For research use only. We do not sell to patients.

CA77.1 Chemical Structure

CA77.1 Chemical Structure

CAS No. : 2412270-22-3

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

In Vitro

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[1].
CA77.1 (20 μM; 6 hours) does not alter on LC3-II expression, and does not effects autophagic flux in NIH 3T3 cells[1].

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

In Vivo

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[1].
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[1].

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

Animal Model: 9-month-old CTR or PS19 mice[1]
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.
Molecular Weight

297.74

Formula

C₁₆H₁₂ClN₃O

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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Keywords:

CA77.1AutophagyCMAalzheimer's?diseaseADLAMP2AneuropathologyderivativeKFERQInhibitorinhibitorinhibit

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