1. Autophagy
  2. Autophagy
  3. CA77.1

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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 352 In-stock
100 mg USD 550 In-stock
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Based on 2 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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

Off-white to light yellow

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, 2 years; -20°C, 1 year (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (16.79 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  45% PEG300    5% Tween-80    50% Saline

    Solubility: 2 mg/mL (6.72 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3586 mL 16.7932 mL 33.5864 mL 83.9659 mL
5 mM 0.6717 mL 3.3586 mL 6.7173 mL 16.7932 mL
10 mM 0.3359 mL 1.6793 mL 3.3586 mL 8.3966 mL
15 mM 0.2239 mL 1.1195 mL 2.2391 mL 5.5977 mL
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CA77.1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CA77.1
Cat. No.:
HY-134923
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