| 产品描述： | AT-56 是一种口服活性的 lipocalin-type prostaglandin (PG) D synthase (L-PGDS) 的选择性抑制剂，对应的Ki值和IC50值分别为75 μM和95 μM |
| 靶点： |
L-PGDS (Cell-free assay):75 μM(Ki);L-PGDS(Cell-free assay):95 μM;PGESynthase |
| 体内研究： |
Orally administered AT-56 (<30 mg/kg body weight) decreases the PGD2 production to 40% in the brain of H-PGDS-deficient mice after a stab wound injury in a dose-dependent manner without affecting the production of PGE2 and PGF2α and also suppresses the accumulation of eosinophils and monocytes in the bronco-alveolar lavage fluid from the antigen-induced lung inflammation model of human L-PGDS-transgenic mice. |
| 细胞实验： |
Cell lines: TE-671 cells, MEG-01S cells Concentrations: 0 - 100 μM Incubation Time: 10 min Method: TE-671 (1×106 cells/well) and MEG-01S (5×105 cells/well) are seeded into multiplates and cultured in Dulbecco's modified Eagle's medium supplemented with 10% heat-inactivated fetal bovine serum, 4 mM L-glutamine, 4.5 g/liter glucose, 100 units/ml penicillin, and 100 μg/ml streptomycin sulfate under a 5% CO2 atmosphere at 37 ℃. MEG-01S cells are caused to differentiate by treatment with 12-O-tetradecanoylphorbol-13-acetate to express H-PGDS and COX-1. After the cells have been cultured for 1 day, AT-56 is added to them at different doses ranging from 0 to 100 μM, and the cells are then incubated at 37 ℃ for 10 min. Thereafter, they are stimulated with a calcium ionophore, A23187 (5 μM), at 37 ℃ for 15 min. The culture media were harvested and centrifuged at 10,000 × g for 5 min to remove the cells, and the supernatant is removed and stored at 80 ℃ until the measurements of PGs can be made. |
| 动物实验： |
Animal Models: H-PGDS KO mice (14–16-week-old males or females weighing 25–30 g, C57BL/6 strain) Dosages: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Oral gavage |
| 参考文献： |
1. Daisuke Irikura, et al. J Biol Chem. 2009 Mar 20;284(12):7623-30. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.516 ml |
12.578 ml |
25.156 ml |
| 5 mM |
0.503 ml |
2.516 ml |
5.031 ml |
| 10 mM |
0.252 ml |
1.258 ml |
2.516 ml |
| 50 mM |
0.05 ml |
0.252 ml |
0.503 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京