AT 56
目录号 : GC11950
AT 56是一种口服有效的脂钙蛋白型前列腺素D合成酶（L-PGDS）选择性抑制剂，IC50值为95µM。
Cas No.:162640-98-4
Sample solution is provided at 25 µL, 10mM.
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AT 56 is an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 value of 95µM[1]. AT 56 can inhibit leptin production and PGD2 production and affect cell proliferation[2]. AT 56 has been widely used to regulate the endothelial-to-mesenchymal transition (EndMT) process in cancer cell models[3].
In vitro, AT 56 treatment (100µM) for 48h inhibited cell proliferation and c-myc expression in diffuse large B-cell lymphoma (DLBCL) cells[4]. Treatment with 5µM AT 56 for 7 days significantly inhibited the development of wild-type oligodendrocytes without affecting cell survival[5]. Treatment with 5µM AT 56 for 10min inhibited PGD2 production in TE671 cells cultured under serum starvation conditions[6].
In vivo, AT 56 treatment via oral administration at a dose of 30mg/kg/day for 4 weeks reduced the ethanol-induced increase in vascular branching in the cerebral cortex of C57BL/6J mice and decreased L-PGDS expression[7]. Intraperitoneal injection of AT 56 (10mg/kg/day) for 7 days partially rescued the reproductive dysfunction of Clpxfl/fl; Zp3-Cre mice by inhibiting PGD2 synthesis[8].
References:
[1] 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[J]. Journal of Biological Chemistry, 2009, 284(12): 7623-7630.
[2] Urade Y. Biochemical and structural characteristics, gene regulation, physiological, pathological and clinical features of lipocalin-type prostaglandin D2 synthase as a multifunctional lipocalin[J]. Frontiers in Physiology, 2021, 12: 718002.
[3] Omori K, Morikawa T, Kunita A, et al. Lipocalin-type prostaglandin D synthase‐derived PGD2 attenuates malignant properties of tumor endothelial cells[J]. The Journal of pathology, 2018, 244(1): 84-96.
[4] Hu S, Ren S, Cai Y, et al. Glycoprotein PTGDS promotes tumorigenesis of diffuse large B-cell lymphoma by MYH9-mediated regulation of Wnt–β-catenin–STAT3 signaling[J]. Cell Death & Differentiation, 2022, 29(3): 642-656.
[5] Pan L, Trimarco A, Zhang A J, et al. Oligodendrocyte-lineage cell exocytosis and L-type prostaglandin D synthase promote oligodendrocyte development and myelination[J]. Elife, 2023, 12: e77441.
[6] Fujimori K, Aritake K, Urade Y. Enhancement of prostaglandin D2 production through cyclooxygenase-2 and lipocalin-type prostaglandin D synthase by upstream stimulatory factor 1 in human brain-derived TE671 cells under serum starvation[J]. Gene, 2008, 426(1-2): 72-80.
[7] Li J, Li C, Subedi U, et al. The Role of Endothelial L-PGDS in the Pro-Angiogenic and Anti-Inflammatory Effects of Low-Dose Alcohol Consumption[J]. Cells, 2024, 13(23): 2007.
[8] Hua R, Hai Z, Gu J, et al. AT-56 RESCUES OOCYTE DYSFUNCTION IN OOCYTE-SPECIFIC KNOCKOUT CLPX MICE BY INHIBITING PGD2 SYNTHESIS[J]. Fertility and Sterility, 2024, 122(4): e171.
AT 56是一种口服有效的脂钙蛋白型前列腺素D合成酶（L-PGDS）选择性抑制剂，IC50值为95µM[1]。AT 56能够抑制瘦素产生和PGD2合成，并影响细胞增殖[2]。AT 56已广泛应用于癌细胞模型中调控内皮-间质转化过程[3]。
在体外，使用100µM的AT 56处理弥漫大B细胞淋巴瘤(DLBCL)细胞48小时，可抑制细胞增殖并降低c-myc表达[4]。用5µM的AT 56处理野生型少突胶质细胞7天，能显著抑制其发育过程而不影响细胞存活[5]。在血清饥饿条件下培养的TE671细胞中，5µM的AT 56处理10分钟即可抑制PGD2的生成[6]。
在体内，通过每日口服30mg/kg/day剂量的AT 56连续4周，可减轻乙醇诱导的C57BL/6J小鼠大脑皮层血管分支增生，并降低L-PGDS表达[7]。每日腹腔注射10mg/kg/day剂量的AT 56（连续7天），能通过抑制PGD2合成，部分挽救Clpxfl/fl; Zp3-Cre小鼠的生殖功能障碍[8]。
| Cell experiment [1]: | |
Cell lines | TE-671 cells |
Preparation Method | TE-671 cells (1×106 cells/well) were seeded in multi-well plates. Cultures were grown in Dulbecco's modified Eagle medium (DMEM) containing 10% heat-inactivated fetal bovine serum, 4mM glutamine, 4.5g/l glucose, 100U/ml penicillin, and 100μg/ml streptomycin sulfate at 37°C at 5% CO2. After 1 day of cell culture, AT 56 was added at various doses (0, 3, 10, 30, and 100μM), and the cells were then incubated at 37°C for 10min. The amount of PGD2 released from TE-671 cells was measured by enzyme-linked immunosorbent assay. |
Reaction Conditions | 0, 3, 10, 30, and 100μM; 10min |
Applications | AT 56 treatment reduced the the production of PGD2 in a dose-dependent manner within TE-671 cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Sixty-two male C57BL/6J mice (3 months old) (25-30g) were randomly divided into 2 groups and fed with 0.7g/kg ethanol (experimental group) or an equal volume of water (control group) daily for 8 weeks. Mice in the control and experimental groups were orally administered AT 56 (30mg/kg/day) for 4 weeks starting from week 5. At the end of the 8-week feeding period, mice were euthanized to measure cerebral vessel density and L-PGDS expression under physiological conditions. |
Dosage form | 30mg/kg/day for 4 weeks; p.o. |
Applications | AT 56 treatment significantly reduced the alcohol-induced increase in vascular branching within the cerebral cortex and subcortical regions of mice, and decreased L-PGDS expression. |
References: | |
| Cas No. | 162640-98-4 | SDF | |
| 化学名 | 1-(4-(2H-tetrazol-5-yl)butyl)-4-(5H-dibenzo[a,d][7]annulen-5-ylidene)piperidine | ||
| Canonical SMILES | N(CC/1)(CCCCC2=NNN=N2)CCC1=C3C4=CC=CC=C4C=CC5=CC=CC=C\35 | ||
| 分子式 | C25H27N5 | 分子量 | 397.52 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5156 mL | 12.578 mL | 25.156 mL |
| 5 mM | 503.1 μL | 2.5156 mL | 5.0312 mL |
| 10 mM | 251.6 μL | 1.2578 mL | 2.5156 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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