- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)