| 货号 | 13160-50mg |
| 描述 | Prostaglandin D synthase (PGDS) catalyzes the isomerization of PGH2 to produce PGD2. PGD2 induces sleep, regulates nociception, inhibits platelet aggregation, and acts as an allergic mediator. Two distinct types of PGDS have been identified, namely the lipocalin-type enzyme (β-trace, L-PGDS) and the hematopoietic-type enzyme (H-PGDS).1,2,3 L-PGDS is localized in the central nervous system, male genital organs of various mammals, and the human heart and is a major protein in human cerebrospinal fluid (CSF).1 AT-56 is a selective, competitive, and highly bioavailable inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS) with a Ki value of 75 µM.4 It inhibits the production of PGD2 by L-PGDS-expressing cells purified from human CSF and recombinant mouse cells with an IC50 value of 95 µM.4 At concentrations as high as 100 µM in vitro or 30 mg/kg in vivo, AT-56 does not affect the production of PGE2, PGF2α, or H-PGDS-catalyzed PGD2.4 At 10 mg/kg AT-56, the numbers of total cells, infiltrating eosinophils, and monocytes in bronchoalveolar lavage fluid of L-PGDS transgenic mice were decreased to 23, 6, and 41% of controls, respectively.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Urade, Y.,Watanabe, K., and Hayaishi, O. Prostaglandin D, E, and F synthases. Journal of Lipid Mediators and Cell Signalling 12, 257-273 (1995). 2.Urade, Y., and Hayaishi, O. Prostaglandin D synthase: Structure and function. Vitamins and Hormones 58, 89-120 (2000). 3.Urade, Y., and Eguchi, N. Lipocalin-type and hematopoietic prostaglandin D synthases as a novel example of functional convergence. Prostaglandins & Other Lipid Mediators 68-69, 375-382 (2002). 4.Irikura, D.,Aritake, K.,Nagata, N., et al. Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase. The Journal of Biological Chemisty 284(12), 7623-7630 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 397.5 |
| 分子式 | C25H27N5 |
| CAS号 | 162640-98-4 |
| 稳定性 | ≥ 2 years |
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