BAY-678
目录号 : GC12088
A selective, cell permeable inhibitor of human neutrophil elastase
Cas No.:675103-36-3
Sample solution is provided at 25 µL, 10mM.
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BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE) [1][2].
Human neutrophil elastase (HNE) is a member of the chymotrypsin-like family of serine proteases and is stored in the neutrophil cytoplasm. HNE is a key protease for matrix degradation and high HNE activity is occured in inflammatory diseases. So HNE is a potential target for the treatment of pulmonary diseases such as acute lung injury (ALI), acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease (COPD), bronchiectasis (BE), and pulmonary hypertension (PH) [1].
BAY-678 is an orally active, potent and selective inhibitor of human neutrophil elastase (HNE). BAY-678 inhibited HNE reversibly with IC50 value of 20 nM and Ki value of 15 nM. BAY-678 showed no inhibition against 21 related serine proteases, up to a concentration of 30 μM [1].
In rats, BAY-678 showed medium clearance with t1/2 of 1.3h [1].
References:
[1]. von Nussbaum F, Li VM, Allerheiligen S, et al. Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.
[2]. von Nussbaum F, Li VM, Meibom D, et al. Potent and Selective Human Neutrophil Elastase Inhibitors with Novel Equatorial Ring Topology: in vivo Efficacy of the Polar Pyrimidopyridazine BAY-8040 in a Pulmonary Arterial Hypertension Rat Model. ChemMedChem. 2016 Jan 19;11(2):199-206.
| Cas No. | 675103-36-3 | SDF | |
| 化学名 | 5-[(4R)-5-acetyl-1,2,3,4-tetrahydro-6-methyl-2-oxo-1-[3-(trifluoromethyl)phenyl]-4-pyrimidinyl]-2-pyridinecarbonitrile | ||
| Canonical SMILES | O=C1N(C2=CC(C(F)(F)F)=CC=C2)C(C)=C(C(C)=O)[C@@H](C3=CN=C(C#N)C=C3)N1 | ||
| 分子式 | C20H15F3N4O2 | 分子量 | 400.4 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at 2°C to 8°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 | 2.4975 mL | 12.4875 mL | 24.975 mL |
| 5 mM | 0.4995 mL | 2.4975 mL | 4.995 mL |
| 10 mM | 0.2498 mL | 1.2488 mL | 2.4975 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet