| 产品描述: | HDAC6 选择性抑制剂;HDAC6 Selective Inhibitors;;InformationACY-775 is a potent and selectivehistone deacetylase 6 (HDAC6)inhibitor with IC50 of 7.5 nM.TargetsHDAC6 (Cell-free assay) 7.5 nM |
| 体内研究: |
Biodistribution profiles of ACY-738, ACY-775, and tubastatin A 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-738 and ACY-775 are 515 ng/mL (1.9 μM) and 1359 ng/mL (4.1 μM). Elimination from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/mL after 2 h. Nevertheless, areas under concentration time curves for brain and plasm calculated over 2 h for both ACY-738 and ACY-775 lead to ratios >1. When ACY-738 (5 mg/kg) or ACY-775 (50 mg/kg) are 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. |
| 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. 3. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.027 ml |
15.135 ml |
30.27 ml |
| 5 mM |
0.605 ml |
3.027 ml |
6.054 ml |
| 10 mM |
0.303 ml |
1.514 ml |
3.027 ml |
| 50 mM |
0.061 ml |
0.303 ml |
0.605 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |