AT 56 |
カタログ番号GC11950
One-Click Copy Product Info
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AT 56はリポカリン型プロスタグランジンD合成酵素(L-PGDS)の経口活性と選択的な阻害剤であり、IC50値は95µMである。
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はリポカリン型プロスタグランジンD合成酵素(L-PGDS)の経口活性と選択的な阻害剤であり、IC50値は95µMである[1]。AT 56はレプチンの産生とPGD2の産生を阻害し、細胞の増殖を影響できる[2]。AT 56は、癌細胞モデルで、内皮間葉転換（EndMT）のプロセスの制御に広く使われている[3]。
体外で、48時間のAT 56(100µM)処理は、瀰漫性大細胞型B細胞リンパ腫（DLBCL）細胞で、細胞の増殖とc-mycの発見を阻害した[4]。5µM AT 56の7日間の処理は、細胞の生存率を影響せずに、野生型オリゴデンドロサイトの成長を著しく阻害した[5]。5µM AT 56の10分間の処理は、血清飢餓条件下のTE671細胞で、PGD2の生産を阻害した[6]。
体内で、30mg/kg/日のAT 56を4週間経口投与した結果、C57BL/6Jマウスの大脳皮質の血管分岐のエタノール誘発の増加を減らし、L-PGDSの発見を減らした[7]。AT 56 (10mg/kg/日)を7日間腹腔内注射した結果、PGD2合成を阻害することで、Clpxfl/fl; Zp3-Creマウスの生殖機能障害を部分的に回復させられる[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.
| 細胞実験[1]: | |
細胞株 | TE-671細胞 |
準備方法 | TE-671細胞（1×106個の細胞/ウェル）をマルチウェルのプレートに播種した。37°C、5% CO2で、10%の加熱不活化牛胎児血清、4mMのグルタミン、4.5g/lのグルコース、100U/mlのペニシリン、100μg/mlのストレプトマイシン硫酸塩を含有するDulbecco's修飾Eagle培地(DMEM)で培養した。1日間の細胞培養後、様々な用量（0、3、10、30と100μM）でAT 56を添加し、その後、37℃で細胞を10分間インキュベートした。TE-671細胞から放出されたPGD2の量を、酵素結合の免疫吸着法で測定した。 |
反応条件 | 0、3、10、30と100μM；10分間 |
アプリケーション | TE-671細胞内で、AT 56の処理は、PGD2の産生を用量依存的に減らした。 |
| 動物実験 [2]: | |
動物モデル | C57BL/6Jマウス |
準備方法 | 62匹の雄のC57BL/6Jマウス(3か月齢) (25-30g)をランダムに2つのグループに分け、0.7g/kgのエタノール（実験群）または等量の水（対照群）を8週間毎日投与した。対照群と実験群のマウスには、5週目から、AT 56 (30mg/kg/日)を4週間経口投与した。8週間の飼育期の終わりに、マウスを安楽死させ、生理学的条件下で、脳血管密度とL-PGDS発見を測定した。 |
投与形態 | 30mg/kg/日、4週間；経口投与 |
アプリケーション | AT 56の処理は、マウスの大脳皮質と皮質下領域内で、血管分岐のアルコール誘発の増加を著しく減らし、L-PGDSの発見を減らした。 |
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 |
| 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 | 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. |
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| 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)