ACY-775
目录号 : GC30782An HDAC6 inhibitor
Cas No.:1375466-18-4
Sample solution is provided at 25 µL, 10mM.
ACY-775 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 0.0075 ?M).1 It is selective for HDAC6 over HDAC1, HDAC2, and HDAC3 (IC50s = 2.1, 2.5, and 11.2 ?M, respectively). ACY-775 (2.5 ?M) increases α-tubulin acetylation at lysine 40 in RN46A-B14 serotonergic cells. It increases the distance traveled in the center of the open field test and decreases immobility time in the tail suspension test, indicating anxiolytic- and antidepressant-like activities, respectively, in mice when administered at a dose of 50 mg/kg.
1.Jochems, J., Boulden, J., Lee, B.G., et al.Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailabilityNeuropsychopharmacology39(2)389-400(2014)
Cell experiment: | Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, 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 histone extraction kit and quantified using protein assay. |
Animal experiment: | 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. Activity is recorded[2]. |
References: [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. |
Cas No. | 1375466-18-4 | SDF | |
Canonical SMILES | O=C(NO)C(C=N1)=CN=C1NC2(CCCCC2)C3=CC=CC(F)=C3 | ||
分子式 | C17H19FN4O2 | 分子量 | 330.36 |
溶解度 | DMSO : 100 mg/mL (302.70 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.027 mL | 15.135 mL | 30.27 mL |
5 mM | 0.6054 mL | 3.027 mL | 6.054 mL |
10 mM | 0.3027 mL | 1.5135 mL | 3.027 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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