HA-155
(Synonyms: Autotaxin Inhibitor IV) 目录号 : GC10869
A selective autotaxin inhibitor
Cas No.:1229652-22-5
Sample solution is provided at 25 µL, 10mM.
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IC50 = 5.7 nM
HA155 is an autotaxin inhibitor.
Autotaxin (ATX), a secreted phosphodiesterase, hydrolyzes the abundant phospholipid lysophosphatidylcholine (LPC) to produce lysophosphatidic acid (LPA). The ATX-LPA signaling axis has been reported to be involved in fibrosis, inflammation, and tumor progression, rendering ATX an attractive drug target.
In vitro: HA155 was identified as a boronic acid-based inhibitor of ATX based on the crystal structure of ATX in complex with HA155. Furthermore, the syntheses and activities of HA155 could be explained by structural data. In order to further understand the difference in activity, molecular docking experiments were performed. The molecular docking indicated a remarkable binding pose for one of the isomers, which differed from the original binding pose of HA155 for ATX. Moreover, the thrombin-mediated increase in platelet-derived LPA was completely attenuated in a dose-dependent manner by HA155. HA-155 could inhibit autotaxin by selectively binding to its catalytic threonine. HA155 showed to dose-dependently block thrombin-induced LPA secretion in platelets [1,2].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Albers, H. M.H.G.,Hendrickx, L.J.D.,van Tol, R.J.P., et al. Structure-based design of novel boronic acid-based inhibitors of autotaxin. Journal of Medicinal Chemistry 54(13), 4619-4626 (2011).
[2] Fulkerson, Z. ,Wu, T.,Sunkara, M., et al. Binding of autotaxin to integrins localizes lysophosphatidic acid production to platelets and mammalian cells. The Journal of Biological Chemisty 286(40), 34654-34663 (2011).
| Cas No. | 1229652-22-5 | SDF | |
| 别名 | Autotaxin Inhibitor IV | ||
| 化学名 | B-[4-[[4-[[3-[(4-fluorophenyl)methyl]-2,4-dioxo-5-thiazolidinylidene]methyl]phenoxy]methyl]phenyl]-boronic acid | ||
| Canonical SMILES | FC1=CC=C(CN2C(/C(SC2=O)=C/C3=CC=C(OCC4=CC=C(B(O)O)C=C4)C=C3)=O)C=C1 | ||
| 分子式 | C24H19BFNO5S | 分子量 | 463.3 |
| 溶解度 | ≤30mg/ml in DMSO;50mg/ml in dimethyl formamide | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1584 mL | 10.7921 mL | 21.5843 mL |
| 5 mM | 0.4317 mL | 2.1584 mL | 4.3169 mL |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1584 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet