BI-2545
目录号 : GC60074
An inhibitor of autotaxin
Cas No.:2162961-71-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BI-2545 is an inhibitor of autotaxin (IC50s = 2.2 and 3.4 for the human and rat enzyme, respectively).1 It is selective for autotaxin over a panel of 48 enzymes, transporters, ion channels, and receptors at 10 ?M. BI-2545 (10 mg/kg) reduces plasma lysophosphatidic acid (LPA) levels in rats.
1.Kuttruff, C.A., Ferrara, M., Bretschneider, T., et al.Discovery of BI-2545: A novel autotaxin inhibitor that significantly reduces LPA levels in vivoACS Med. Chem. Lett.8(12)1252-1257(2017)
| Cas No. | 2162961-71-7 | SDF | |
| Canonical SMILES | O=C(N1C[C@]2([H])[C@H](CNC(C3=CC=C(NN=N4)C4=C3)=O)[C@]2([H])C1)OCC5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5 | ||
| 分子式 | C23H19F6N5O3 | 分子量 | 527.42 |
| 溶解度 | DMSO: 250 mg/mL (474.01 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.896 mL | 9.4801 mL | 18.9602 mL |
| 5 mM | 0.3792 mL | 1.896 mL | 3.792 mL |
| 10 mM | 0.1896 mL | 0.948 mL | 1.896 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。
Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo
ACS Med Chem Lett 2017 Nov 8;8(12):1252-1257.PMID:29259743DOI:PMC5733304
In an effort to find new therapeutic interventions addressing the unmet medical need of patients with idiopathic pulmonary fibrosis, we initiated a program to identify new autotaxin (ATX) inhibitors. Starting from a recently published compound (PF-8380), we identified several highly potent ATX inhibitors with improved pharmacokinetic and safety profiles. Further optimization efforts resulted in the identification of a single-digit nanomolar lead compound (BI-2545) that shows substantial lowering of LPA in vivo and is therefore considered a valuable tool for further studies.