BAY-X 1005
(Synonyms: BAY X 1005; DG-031) 目录号 : GC12232
BAY-X 1005 (BAY X 1005; DG-031) 是一种具有口服活性的选择性 5-脂氧合酶活化蛋白 (FLAP) 抑制剂。
Cas No.:128253-31-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BAY-X 1005 is a selective inhibitor of 5-lipoxygenase-activating protein [1].
5-lipoxygenase-activating protein (FLAP) is an integral protein and plays an important role in the activation of 5-lipoxygenase (5-LOX) and the synthesis of leukotrienes, which regulating immune responses.
BAY-X 1005 is a selective inhibitor of leukotriene synthesis. BAY X 1005 binds to FLAP and inhibits 5-LOX translocation from the cytosol to membranes [1]. BAY-X1005 inhibited LTB4 synthesis with IC50 values of 0.22, 0.026 and 0.039 μM for isolated PMNL of human, rat and mouse respectively and inhibited LTC4 synthesis with IC50 value of 0.021 μM in mouse macrophages [2].
In the arachidonate-induced mouse ear inflammation test, BAY-X 1005 inhibited myeloperoxidase activity and edema formation with ED50 values of 7.9 and 48.7, respectively [2].
Also, BAY-X 1005 (100 mg/kg) reduced platelet-activating factor-induced death of mice by 51% in a dose-dependent way. In animal models, BAY-X 1005 inhibited the synthesis of LTB4 and LTC4, which reduced edema formation, the vascular phenomena of inflammation and leukocyte immigration [3].
References:
[1]. Hatzelmann A, Fruchtmann R, Mohrs KH, et al. Mode of action of the leukotriene synthesis (FLAP) inhibitor BAY X 1005: implications for biological regulation of 5-lipoxygenase. Agents Actions, 1994, 43(1-2): 64-68.
[2]. Müller-Peddinghaus R, Fruchtmann R, Ahr HJ, et al. BAY X1005, a new selective inhibitor of leukotriene synthesis: pharmacology and pharmacokinetics. J Lipid Mediat, 1993, 6(1-3): 245-248.
[3]. Müller-Peddinghaus R, Kohlsdorfer C, Theisen-Popp P, et al. BAY X1005, a new inhibitor of leukotriene synthesis: in vivo inflammation pharmacology and pharmacokinetics. J Pharmacol Exp Ther, 1993, 267(1): 51-57.
| Cas No. | 128253-31-6 | SDF | |
| 别名 | BAY X 1005; DG-031 | ||
| 化学名 | (S)-2-cyclopentyl-2-(4-(quinolin-2-ylmethoxy)phenyl)acetic acid | ||
| Canonical SMILES | OC([C@H](C(C=C1)=CC=C1OCC2=NC3=CC=CC=C3C=C2)C4CCCC4)=O | ||
| 分子式 | C23H23NO3 | 分子量 | 361.43 |
| 溶解度 | <36.14mg/ml in DMSO | 储存条件 | Store at RT |
| 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 | 2.7668 mL | 13.8339 mL | 27.6679 mL |
| 5 mM | 0.5534 mL | 2.7668 mL | 5.5336 mL |
| 10 mM | 0.2767 mL | 1.3834 mL | 2.7668 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。