S86564 |
AR7 |
源叶(MedMol) | 97%(HPLC) |
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- 产品描述: AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy
- 靶点: RAR/RXR;RetinoidReceptor
- 体外研究:
Treatment with RARA antagonist, AR7 (20 μM; for 16 h), increased lysosomal activity in WT and LRRK2R1441G KI mutant MEFs. AR7 (10, 20, 30 uM; 12, 24 hours) has no effect on macroautophagy in NIH 3T3 cells. Chaperone-mediated autophagy (CMA) contributes to cellular quality control and the cellular response to stress through the selective degradation of cytosolic proteins in lysosomes. Decrease in CMA activity occurs in aging and in age-related disorders. Signaling through the retinoic acid receptor alpha (RARα) inhibits CMA. AR7 significantly activates CMA activity in mouse fibroblasts. A marked increase in CMA-activating potency is found when AR7 and GR1 are combined, supporting their cooperative effect. Treatment with the transcriptional repressor Actinomycin D partially reduces the stimulatory effect of AR7 on CMA, consistent with transcriptional changes contributing to the upregulation of CMA
- 参考文献:
1. Philip Wing-Lok Ho, 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 Feb;16(2):347-370. 2. Mathieu Bourdenx, et al. Chaperone-mediated autophagy prevents collapse of the neuronal metastable proteome. Cell. 2021 May 13;184(10):2696-2714.e25. 3. Anguiano J, et al. Chemical modulation of chaperone-mediated autophagy by retinoic acid derivatives. Nat Chem Biol. 2013 Jun;9(6):374-82.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.88 ml 19.401 ml 38.803 ml 5 mM 0.776 ml 3.88 ml 7.761 ml 10 mM 0.388 ml 1.94 ml 3.88 ml 50 mM 0.078 ml 0.388 ml 0.776 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)