AT 56 |
| Catalog No.GC11950 |
AT 56은 95μM의 IC50 및 75μM의 Ki를 갖는 리포칼린형 프로스타글란딘 D 합성효소(L-PGDS)의 강력하고 선택적인 경구 활성 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Chemical Name | 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 | ||
| Formula | C25H27N5 | M.Wt | 397.52 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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