CA77.1 |
Catalog No.GC62881
One-Click Copy Product Info
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CA77.1 is an orally active small-molecule derivative of 7-chloro-3-(p-tolyl)-2H-benzo[b]oxazine (AR7) and can act as an activator of chaperone-mediated autophagy (CMA).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2412270-22-3
Sample solution is provided at 25 µL, 10mM.
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CA77.1 is an orally active small-molecule derivative of 7-chloro-3-(p-tolyl)-2H-benzo[b][1,4]oxazine (AR7) and can act as an activator of chaperone-mediated autophagy (CMA)[1]. CA77.1 exerts neuroprotective effects and is being developed for the treatment of various chronic CNS diseases including Alzheimer's disease, Parkinson’s disease and retinal degeneration[2].
In vitro, CA77.1 (12μM) pretreated murine microglial BV2 cells for 12h followed by LPS treatment. CA77.1 decreased LPS-induced iNOS and COX-2 protein expression, lowered the proinflammatory factors NO and IL-6 and reduced the mRNA expression of iNOS, COX-2, IL-6, and IL-1β without affecting cell viability[3]. CA77.1 (20µM) treatment on mouse neuroblast Neuro-2a (N2a) cells for 24h promoted the degradation of GAPDH (a canonical substrate of CMA) and augmented Na+ /K+ -ATPase β1 subunit elimination, accompanied by decreased Na+ /K+ -ATPase activity and increased concentration of intracellular Na+, without mRNA levels changed[4]. CA77.1 (0-30μM) treatment on PK-15 porcine kidney cells expressing foot-and-mouth disease virus (FMDV) non-structural protein 3D for 24h effectively diminished FMDV 3D polymerase levels and suppressesd FMDV replication via activation of the CMA pathway[5].
In vivo, CA77.1 (10mg/kg/day) was intraperitoneally injected into intracerebral hemorrhage (ICH) mice models for six consecutive days. CA77.1 administration reversed ICH induced augmentation of A1 reactive astrocytes, myelin damage, neuronal death, and neurobehavioral disorders[6]. CA77.1 (10mg/kg) was administered intraperitoneally into mitochondrial toxin BDE-47-exposed mice with cognitive impairment every three days for 4 weeks. CA77.1 mitigated BDE-47-induced cognitive impairment in mice by suppressing ferroptosis, preventing synaptic loss in mice hippocampi and rescuing hippocampal neuronal structural atrophy[7].
References:
[1] Bourdenx M, Martín-Segura A, Scrivo A, et al. Chaperone-mediated autophagy prevents collapse of the neuronal metastable proteome.Cell. 2021 May 13;184(10):2696-2714.e25.
[2] Wu J, Xu W, Su Y, et al. Targeting chaperone-mediated autophagy in neurodegenerative diseases: mechanisms and therapeutic potential.Acta Pharmacol Sin. 2025 Apr;46(4):816-828.
[3] Wu J, Han Y Y, Xu H, et al. Deficient chaperone-mediated autophagy facilitates LPS-induced microglial activation via regulation of the p300/NF-κB/NLRP3 pathway. Sci Adv. 2023 Oct 6;9(40):eadi8343.
[4] Zhang Y X, Wu H H, Zhang Q, et al. LAMP2A-mediated neuronal hyperexcitability by enhancing NKAβ1 degradation underlies depression-induced allodynia. Cell Rep. 2025 Apr 22;44(4):115489.
[5] Ren M, Zhou H Q, Wu J E, et al. Heat shock protein A1 inhibits the replication of foot-and-mouth disease virus by degrading viral RNA polymerase 3D through chaperone-mediated autophagy. J Virol. 2025 May 20;99(5):e0016825.
[6] Zheng Y, Peng L, Jiang G N, et al. Activation of chaperone-mediated autophagy exerting neuroprotection effect on intracerebral hemorrhage-induced neuronal injury by targeting Lamp2a. Exp Neurol. 2024 Dec:382:114986.
[7] Yuan Q, Wang M W, Zhang Z X, et al. The ameliorative effects of melatonin against BDE-47-induced hippocampal neuronal ferroptosis and cognitive dysfunction through Nrf2-Chaperone-mediated autophagy of ACSL4 degradation. Ecotoxicol Environ Saf. 2025 Jan 15:290:117542.
| Cell experiment [1]: | |
Cell lines | Murine microglial BV2 cells |
Preparation Method | BV2 cells were pretreated with 12μM CA77.1 for 12h and then exposed to LPS for 10min. |
Reaction Conditions | 12μM; 12h |
Applications | CA77.1 decreased LPS-induced expression of iNOS and COX-2 proteins, lowered the proinflammatory factors NO and IL-6 and reduced the mRNA expression of iNOS, COX-2, IL-6, and IL-1β without affecting cell viability. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Mice were randomly divided into the following groups: control group, 2,2′,4,4′-tetrabromodiphenyl ether (BDE-47) group, BDE-47 + CA77.1 group. BDE-47 group mice were orally administered 20mg/kg/day BDE-47 and also intraperitoneally injected with normal saline containing 2 % DMSO for 8 weeks. BDE-47 + CA77.1 group mice were given an intraperitoneal injection of 10mg/kg CA77.1 every three days for the last 4 weeks prior to 20mg/kg/day BDE-47 administration. |
Dosage form | 10mg/kg; i.p.; every 3 days for the last 4 weeks |
Applications | CA77.1 mitigated BDE-47-induced cognitive impairment in mice by suppressing ferroptosis, preventing synaptic loss in mice hippocampi and rescuing hippocampal neuronal structural atrophy. |
References: | |
| Cas No. | 2412270-22-3 | SDF | |
| Formula | C16H12ClN3O | M.Wt | 297.74 |
| Solubility | 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) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3586 mL | 16.7932 mL | 33.5864 mL |
| 5 mM | 671.7 μL | 3.3586 mL | 6.7173 mL |
| 10 mM | 335.9 μL | 1.6793 mL | 3.3586 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)