GSK2256294A (GSK 2256294)
(Synonyms: GSK 2256294) 目录号 : GC32455
GSK2256294A (GSK 2256294) (GSK 2256294) 是可溶性环氧化物水解酶 (sEH) 的选择性和口服活性抑制剂。
Cas No.:1142090-23-0
Sample solution is provided at 25 µL, 10mM.
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GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.IC50 value: 27 pMTarget: sEHin vitro: GSK2256294A also displays potent cellular inhibition (IC50 = 0.66 nM) of sEH in an assay developed using a cell line transfected with the human sEH enzyme. [1]in vivo: A novel, potent, selective inhibitor of recombinant human, rat and mouse sEH, GSK2256294A, exhibits potent cell-based activity, a concentration-dependent inhibition of the conversion of 14,15-EET to 14,15-DHET in human, rat and mouse whole blood, and a dose-dependent increase in the LTX/LTX diol ratio in rat plasma following oral administration. Mice receiving 10 days of cigarette smoke exposure concomitant with oral administration of GSK2256294A exhibits significant, dose-dependent reductions in pulmonary leukocytes and keratinocyte chemoattractant levels. Mice receiving oral administration of GSK2256294A following 10 days of cigarette smoke exposure exhibited significant reductions in pulmonary leukocytes compared to vehicle-treated mice.
[1]. Podolin PL, et al. In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid Mediat. 2013 Jul-Aug;104-105:25-31.
| Cas No. | 1142090-23-0 | SDF | |
| 别名 | GSK 2256294 | ||
| Canonical SMILES | O=C([C@H]1C[C@@H](NC2=NC(NC)=NC(C)=N2)CCC1)NCC3=CC=C(C#N)C=C3C(F)(F)F | ||
| 分子式 | C21H24F3N7O | 分子量 | 447.46 |
| 溶解度 | DMSO : ≥ 47 mg/mL (105.04 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 | 2.2348 mL | 11.1742 mL | 22.3484 mL |
| 5 mM | 0.447 mL | 2.2348 mL | 4.4697 mL |
| 10 mM | 0.2235 mL | 1.1174 mL | 2.2348 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet