AR7 |
رقم الكتالوجGC19035
One-Click Copy Product Info
|
AR7 هو مضاد غير نمطي لـ RARA / RARα (مستقبلات حمض الريتينويك ، ألفا)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 80306-38-3
Sample solution is provided at 25 µL, 10mM.
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AR7 is an atypical retinoic acid receptor α (RARα) antagonist [1]. AR7 antagonizes RARα to relieve its inhibition of CMA, thereby significantly enhancing LAMP2A and CMA activity and promoting the selective degradation of misfolded or aggregated proteins [2-3]. AR7 is commonly used to treat Parkinson's disease [4].
In primary cortical neurons, AR7 (0-20μM; 21d) attenuates the progressive accumulation of intracellular and extracellular SNCA oligomers in long-term cultures of cortical neurons [5]. In SN4741 cells, AR7 (20μM; 24h) reduces lipid droplet accumulation in the Wdr45-deficient model by activating chaperone-mediated autophagy (CMA) and promoting the degradation of the lipid biosynthesis enzyme Fasn [6].
In C57BL/6 mice, AR7 (10mg/kg; ip; 6h) alleviates diclofenac-induced hepatic steatosis [7]. In heterozygous offspring mice, administration of AR7 (10mg/kg; ip; 6 weeks) promotes hepatic SERPINA1E342K/ATZ elimination and mitigates hepatic SERPINA1E342K/ATZ aggregation pathology [8].
References:
[1]. Anguiano J, Garner T P, Mahalingam M, et al. Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives[J]. Nature chemical biology, 2013, 9(6): 374-382.
[2]. Bourdenx M, Martín-Segura A, Scrivo A, et al. Chaperone-mediated autophagy prevents collapse of the neuronal metastable proteome[J]. Cell, 2021, 184(10): 2696-2714. e25.
[3]. Wang Y T, Lu J H. Chaperone-mediated autophagy in neurodegenerative diseases: molecular mechanisms and pharmacological opportunities[J]. Cells, 2022, 11(14): 2250.
[4]. Chen J, Mao K, Yu H, et al. p38-TFEB pathways promote microglia activation through inhibiting CMA-mediated NLRP3 degradation in Parkinson's disease[J]. Journal of neuroinflammation, 2021, 18(1): 295.
[5]. Ho P W L, Leung C T, Liu H, et al. Age-dependent accumulation of oligomeric SNCA/α-synuclein from impaired degradation in mutant LRRK2 knockin mouse model of Parkinson disease: role for therapeutic activation of chaperone-mediated autophagy (CMA)[J]. Autophagy, 2020, 16(2): 347-370.
[6]. Xiong Q, Sun H, Wang Y, et al. Lipid droplet accumulation in Wdr45-deficient cells caused by impairment of chaperone-mediated autophagic degradation of Fasn[J]. Lipids in Health and Disease, 2024, 23(1): 91.
[7]. Lee W, Kim H Y, Choi Y J, et al. SNX10-mediated degradation of LAMP2A by NSAIDs inhibits chaperone-mediated autophagy and induces hepatic lipid accumulation[J]. Theranostics, 2022, 12(5): 2351.
[8]. Lin J, Wei X, Dai Y, et al. Chaperone-mediated autophagy degrades SERPINA1E342K/α1-antitrypsin Z variant and alleviates cell stress[J]. Autophagy, 2025: 1-18.
| Cell experiment [1]: | |
Cell lines | Primary cortical neurons |
Preparation Method | To investigate whether AR7 treatment modulates SNCA oligomer levels, mature primary cortical neurons (DIV9) were cultured under normal conditions with or without AR7 (0, 10, or 20μM) for up to 21 days. AR7 dissolved in cell culture-grade DMSO was added to the culture medium at DIV9 and DIV14 at the indicated concentrations. Conditioned medium and total cell lysates were extracted at DIV9, 14, and 21 for Western blotting and SNCA oligomer ELISA analysis. |
Reaction Conditions | 0-20μM; 21d |
Applications | AR7 attenuates the progressive accumulation of intracellular and extracellular SNCA oligomers in long-term cultures of cortical neurons. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Male C57BL/6 mice (7 weeks old) were housed in an air-conditioned room (24℃) with a 12-hour day/night cycle and allowed free access to water and food for one week. After a one-week acclimation period, the animals were randomly divided into four groups (n=6 mice each): Group 1, vehicle; Group 2, diclofenac; Group 3, AR7; and Group 4, diclofenac + AR7. The vehicle group received an intraperitoneal injection of 0.5% DMSO in saline. The diclofenac group received diclofenac (100mg/kg, intraperitoneally) twice every 12 hours. The AR7 group received AR7 (10mg/kg, intraperitoneally) one hour before diclofenac. The following day, the mice were anesthetized with Zolettiline 50 and sacrificed. |
Dosage form | 10mg/kg; ip; 6h |
Applications | AR7 alleviates diclofenac-induced hepatic steatosis in vivo. |
References: | |
| Cas No. | 80306-38-3 | SDF | |
| Canonical SMILES | CC1=CC=C(C2=NC3=CC=C(Cl)C=C3OC2)C=C1 | ||
| Formula | C15H12ClNO | M.Wt | 257.71 |
| الذوبان | DMSO : 25 mg/mL (97.01 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.8803 mL | 19.4017 mL | 38.8033 mL |
| 5 mM | 776.1 μL | 3.8803 mL | 7.7607 mL |
| 10 mM | 388 μL | 1.9402 mL | 3.8803 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
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)