AT-56
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. AT-56 inhibited human and mouse L-PGDSs in a concentration (3-250 microm)-dependent manner but did not affect the activities of hematopoietic PGD synthase (H-PGDS), cyclooxygenase-1 and -2, and microsomal PGE synthase-1. AT-56 inhibited the L-PGDS activity in a competitive manner against the substrate PGH(2) (K(m) = 14 microm) with a K(i) value of 75 microm but did not inhibit the binding of 13-cis-retinoic acid, a nonsubstrate lipophilic ligand, to L-PGDS.
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化学信息
| 名称 | AT-56 |
|---|---|
| Iupac 化学名称 | 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-piperidine |
| 同义词 | AT-56; AT 56; AT56. |
| 英文同义词 | AT-56; AT 56; AT56. |
| 分子式 | C25H27N5 |
| 分子量 | 397.526 |
| Smile | N1(CCCCC2=NNN=N2)CC/C(CC1)=C3C4=CC=CC=C4C=CC5=CC=CC=C/35 |
| InChiKey | LQNGMDUIRLSESZ-UHFFFAOYSA-N |
| InChi | InChI=1S/C25H27N5/c1-3-9-22-19(7-1)12-13-20-8-2-4-10-23(20)25(22)21-14-17-30(18-15-21)16-6-5-11-24-26-28-29-27-24/h1-4,7-10,12-13H,5-6,11,14-18H2,(H,26,27,28,29) |
| Cas号 | 162640-98-4 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
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| 大货 | 询价 | 询价 | 询价 |
| 纯度 | 98% Min. |
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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. PubMed PMID: 19131342; PubMed Central PMCID: PMC2658056.
2: Le Loupp AG, Bach-Ngohou K, Bourreille A, Boudin H, Rolli-Derkinderen M, Denis MG, Neunlist M, Masson D. Activation of the prostaglandin D2 metabolic pathway in Crohn's disease: involvement of the enteric nervous system. BMC Gastroenterol. 2015 Sep 4;15:112. doi: 10.1186/s12876-015-0338-7. PubMed PMID: 26338799; PubMed Central PMCID: PMC4558965.
3: Huang HL, Huang YC, Lee WY, Yeh CN, Lin KJ, Yu CS. 18F-glutathione conjugate as a PET tracer for imaging tumors that overexpress L-PGDS enzyme. PLoS One. 2014 Aug 11;9(8):e104118. doi: 10.1371/journal.pone.0104118. PubMed PMID: 25111383; PubMed Central PMCID: PMC4128654.
4: Zhao G, Yu R, Deng J, Zhao Q, Li Y, Joo M, van Breemen RB, Christman JW, Xiao L. Pivotal role of reactive oxygen species in differential regulation of lipopolysaccharide-induced prostaglandins production in macrophages. Mol Pharmacol. 2013 Jan;83(1):167-78. doi: 10.1124/mol.112.080762. PubMed PMID: 23071105; PubMed Central PMCID: PMC3533474.
5: Fujimori K, Maruyama T, Kamauchi S, Urade Y. Activation of adipogenesis by lipocalin-type prostaglandin D synthase-generated Δ¹²-PGJ₂ acting through PPARγ-dependent and independent pathways. Gene. 2012 Aug 15;505(1):46-52. doi: 10.1016/j.gene.2012.05.052. PubMed PMID: 22664386.
6: Fujimori K, Aritake K, Urade Y. Enhancement of prostaglandin D(2) production through cyclooxygenase-2 and lipocalin-type prostaglandin D synthase by upstream stimulatory factor 1 in human brain-derived TE671 cells under serum starvation. Gene. 2008 Dec 15;426(1-2):72-80. doi: 10.1016/j.gene.2008.08.023. PubMed PMID: 18817855.
