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CAS No.: 162640-98-4

AT-56 Catalog No. CSN27768

AT 56 is an orally active L-PGDS inhibitor with IC50 value of 95μM. It inhibits the production of PGD2 from PGH2 in vitro, with no effect on PGE2 or PGF2α production.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Prostaglandin (PG) D synthase (PGDS) catalyzes the isomerization of PGH(2) to PGD(2), which acts as an endogenous somnogen and an allergic mediator. There are two distinct types of PGDS: one is lipocalin-type PGDS (L-PGDS) localized in the central nervous system, male genitals, and heart; and the other is hematopoietic PGDS (H-PGDS) in mast cells and Th2 lymphocytes. L-PGDS is the same as beta-trace, a major protein in human cerebrospinal fluid, and is also secreted into the seminal plasma and plasma. The L-PGDS concentration in various body fluids is useful as a marker for various diseases such as renal failure and coronary atherosclerosis. H-PGDS is a cytosolic enzyme and is a member of the Sigma class of glutathione S-transferase^[2]. AT-56 is an orally active and selective inhibitor of L-PGDS. AT-56 inhibited human and mouse L-PGDSs in a concentration (3-250 microm)-dependent manner but did not affect the activities of H-PGDS, cyclooxygenase-1 and -2, and microsomal PGE synthase-1. AT-56 inhibited the production of PGD(2) by L-PGDS-expressing human TE-671 cells after stimulation with Ca(2+) ionophore (5 microm A23187) with an IC(50) value of about 3 microm without affecting their production of PGE(2) and PGF(2alpha) but had no effect on the PGD(2) production by H-PGDS-expressing human megakaryocytes.Orally administered AT-56 (<30 mg/kg body weight) decreased the PGD(2) 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 PGE(2) and PGF(2alpha) and also suppressed 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^[3].
参考文献

[1] Irikura D, Aritake K, Nagata N, Maruyama T, Shimamoto S, Urade Y. Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase. J Biol Chem. 2009 Mar 20;284(12):7623-30. doi: 10.1074/jbc.M808593200. Epub 2009 Jan 8. PMID: 19131342; PMCID: PMC2658056.
[2] Yoshihiro Urade,et al. Functional analyses of lipocalin-type and hematopoietic prostaglandin D synthases. Nihon Yakurigaku Zasshi. 2004 Jan;123(1):5-13.
[3] Irikura D, et, al. Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase. J Biol Chem. 2009 Mar 20; 284(12): 7623-30.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5156 mL
- 12.5781 mL
- 25.1563 mL
- 5 mM
- 0.5031 mL
- 2.5156 mL
- 5.0313 mL
- 10 mM
- 0.2516 mL
- 1.2578 mL
- 2.5156 mL

技术信息

CAS号

162640-98-4

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H27N5

运输

蓝冰

分子量

397.52

别名

溶解度

DMSO	80.0 mg/mL (201.3 mM)
Water	Insoluble
Ethanol	Insoluble

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