AT-56

Territorial Availability: Available through Bertin Technologies only in France

• Synonyms
  • 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-piperidine
• Correlated keywords
  • Prostaglandins D synthases L-PGDS PGD2 lipocalin-type inflammation inhibition inhibitors inhibits PGs eosinophils LPGDs bronchoalveolar lavage fluid Lysosomal Proton Translocating ATPases Vacuolar Proton-Translocating ATPases Vacuolar Membrane H(+)-ATPase Proteins Membrane-Associated Membrane-Associated Proteins Membrane Associated Proteins Tacrolimus Binding Proteins Proteins Rapamycin-Binding Proteins Integral Membrane Membrane Proteins Integral Binding Proteins Rapamycin Rapamycin-Binding Proteins Rapamycin Binding Proteins Protein Integral Membrane Integral Membrane Proteins Vacuolar F(1)F(0) ATPasesLysosomal F(1)F(0) ATPase Integral Membrane Protein Vacuolar F(1)F(0) ATPase Proteins Cell Membrane Protein FK-506-Binding Proteins Cell Surface Protein FK506-Binding FK-506-Binding ProteinFK506 Binding Proteins FK 506 Binding Protein Cell Membrane Proteins FK506-Binding ProteinFK506 Binding Protein Cell Surface Proteins H+-ATPase, Vacuolar Vacuolar H+-ATPase Vacuolar H+ ATPase Proteins Membrane Proteins Vacuolar ATPase Rotamase FKBP V Type ATPase FKBP Rotamase Membrane FKBP
• Product Overview:
  Prostaglandin D synthase (PGDS) catalyzes the isomerization of PGH2 to produce PGD2. PGD2 induces sleep, regulates nociception, inhibits platelet aggregation, and acts as an allergic mediator. Two distinct types of PGDS have been identified, namely the lipocalin-type enzyme (?-trace, L-PGDS) and the hematopoietic-type enzyme (H-PGDS).{8448,9588,12044} L-PGDS is localized in the central nervous system, male genital organs of various mammals, and the human heart and is a major protein in human cerebrospinal fluid (CSF).{8448} 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.{16647} It inhibits the production of PGD2 by L-PGDS-expressing cells purified from human CSF and recombinant mouse cells with an IC50 value of 95 µM.{16647} At concentrations as high as 100 µM in vitro or 30 mg/kg in vivo, AT-56 does not affect the production of PGE2, PGF2?, or H-PGDS-catalyzed PGD2.{16647} At 10 mg/kg AT-56, the numbers of total cells, infiltrating eosinophils, and monocytes in bronchoalveolar lavage fluid of L-PGDS transgenic mice were decreased to 23, 6, and 41% of controls, respectively.{16647}