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CAS No.: 80306-38-3

AR7 Catalog No. CSN22084

Synonyms: Atypical retinoid 7

AR7 is a retinoic acid receptor α (RARα) antagonist.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Retinoic acid (RA), the major bioactive metabolite of retinol or vitamin A, induces a spectrum of pleiotropic effects in cell growth and differentiation that are related to embryonic development and adult physiology. The RA activity is mediated primarily by members of the retinoic acid receptor (RAR) subfamily, namely RARα, RARβ and RARγ, which belong to the nuclear receptor (NR) superfamily of transcription factors^[1]. Atypical retinoid 7 (AR7) is a retinoic acid receptor α (RARα) antagonist and also acts as chaperone-mediated autophagy (CMA) activator. AR7 dose-dependently activates CMA activity in mouse fibroblasts expressing the KFERQ-mcherry1 photoactivable reporter. In Parkinson disease, mutant LRRK2 perturbs chaperone-mediated-autophagy (CMA) to degrade α-synuclein. AR7 treatment in 24 h dose-dependently, induced neuronal LAMP2A transcription and lysosomal activity in mouse embryonic fibroblasts (MEFs). AR7 at 20 μM also attenuated the progressive accumulation of both intracellular and extracellular α-synuclein oligomers in prolonged cultures of mutant cortical neurons (DIV21), indicating that oligomer accumulation can be suppressed by CMA activation^[2].
作用机制AR-7 is docked to a hydrophobic region of the RARα-binding pocket formed by h3, h10 and h12^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02429193	Castration-resistant Prostate ... more >>Cancer Collapse <<	Phase 2	Active, not recruiting	June 2018	Canada, British Columbia ... more >> British Columbia Cancer Agency, Vancouver Cancer Centre Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Ontario Princess Margaret Cancer Centre Toronto, Ontario, Canada, M5G 2M9 Collapse <<

参考文献

[1] di Masi A, Leboffe L, De Marinis E, et al. Retinoic acid receptors: from molecular mechanisms to cancer therapy. Mol Aspects Med. 2015;41:1‐115.
[2] Ho PW, Leung CT, 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). Autophagy. 2020;16(2):347‐370.
[3] Anguiano J, Garner TP, Mahalingam M, Das BC, Gavathiotis E, Cuervo AM. Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives [published correction appears in Nat Chem Biol. 2013 Nov;9(11):746]. Nat Chem Biol. 2013;9(6):374‐382.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8803 mL
- 19.4013 mL
- 38.8026 mL
- 5 mM
- 0.7761 mL
- 3.8803 mL
- 7.7605 mL
- 10 mM
- 0.3880 mL
- 1.9401 mL
- 3.8803 mL

技术信息

CAS号

80306-38-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H12ClNO

运输

蓝冰

分子量

257.71

别名

Atypical retinoid 7

溶解度

DMSO	4.0 mg/mL (15.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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