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ACY-775

ACY-775

产品编号 TQ0074   CAS 1375466-18-4

ACY-775 是一种特异性有效的组蛋白脱乙酰酶 6 抑制剂,IC50值为 7.5 nM。

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ACY-775 Chemical Structure
ACY-775, CAS 1375466-18-4
规格 价格/CNY 货期 数量
1 mg ¥ 393 现货
2 mg ¥ 583 现货
5 mg ¥ 972 现货
10 mg ¥ 1,620 现货
25 mg ¥ 3,350 现货
50 mg ¥ 4,880 现货
100 mg ¥ 6,990 现货
500 mg ¥ 14,000 现货
1 mL * 10 mM (in DMSO) ¥ 1,060 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: ACY-775 (TQ0074)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 ACY-775 is an effective and specific inhibitor of HDAC6 (IC50: 7.5 nM).
靶点活性 HDAC6:7.5 nM, HDAC1:2123 nM
体外活性 Upon treatment with ACY-775, a clear enhancement of the acetylation of α-tubulin is visible, while histone acetylation remains unaltered. Acetylation of α-tubulin is visualized by immunofluorescence and the intensity in the neurites of the neurons is quantified and normalized to the length of the fluorescent signal. In vehicle-treated DRG neurons, acetylated α-tubulin is already present. Upon treatment with ACY-775, the signal intensity of acetylated α-tubulin increases significantly. A significant increase in motility of mitochondria and also the total number of mitochondria within the neurites are observed compared with vehicle-treated DRG neurons. A significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compared with vehicle-treated cells [1].
体内活性 Biodistribution profiles of ACY-775 are examined after acute dosing at 5 or 50?mg/kg over 2?h. At t=30?min after acute 50?mg/kg injection, respective plasma levels of ACY-775 is 1359?ng/mL (4.1?μM). Elimination from the plasma is rapid, with a plasmatic half-life of 12?min and a concentration below 10?ng/mL after 2?h. When ACY-775 (50?mg/kg) is administered repeatedly in wild-type mice at 24?h, 4?h, and 30?min before killing, significant increases in α-tubulin acetylation are observed in all tested brain regions [2].
细胞实验 Undifferentiated RN46A-B14 cells are grown. They are treated with 2.5?μM ACY-738, ACY-775, tubastatin A, 0.6?μM TSA or vehicle (0.1% DMSO) for 4?h. Samples are processed using a histone extraction kit and quantified using protein assay [2].
动物实验 Mice are tested for immobility in the TST. At 30?min or 2?h after i.p. injection of ACY-738 (5, 50?mg/kg), ACY-775 (5, 50?mg/kg), and citalopram (0.5, 2, 20?mg/kg), a combination of the previous, or vehicle, mice are attached to the test rig and time immobile over 6?min is recorded. For open-field activity, mice are injected with ACY-738 or ACY-775 at 5, 10, or 50?mg/kg or vehicle and allowed to explore [2].
分子量 330.36
分子式 C17H19FN4O2
CAS No. 1375466-18-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (302.70 mM), Sonification and heating are recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.027 mL 15.135 mL 30.27 mL 75.675 mL
5 mM 0.6054 mL 3.027 mL 6.054 mL 15.135 mL
10 mM 0.3027 mL 1.5135 mL 3.027 mL 7.5675 mL
20 mM 0.1514 mL 0.7568 mL 1.5135 mL 3.7838 mL
50 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5135 mL
100 mM 0.0303 mL 0.1514 mL 0.3027 mL 0.7568 mL

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TargetMol Library Books参考文献

1. Veronick Benoy, et al. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr; 14(2): 417-428. 2. Jeanine Jochems et al. Antidepressant-Like Properties of Novel HDAC6-Selective Inhibitors with Improved Brain Bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2): 389-400.
HDAC-IN-52 Tacedinaline Domatinostat tosylate ITSA-1 Methyl L-histidinate dihydrochloride Sodium 4-phenylbutyrate Parthenolide NKL 22

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 表观遗传库 染色质修饰分子库 细胞重编程化合物库 NF-κB 通路分子库 NO PAINS 化合物库 抗乳腺癌化合物库 经典已知活性库 抗胰腺癌化合物库 DNA 损伤和修复分子库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

ACY-775 1375466-18-4 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases inhibit ACY 775 Inhibitor ACY775 inhibitor

 

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