AT 56L-PGDS inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity ≥95.00%
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Chemical structure
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Cas No. | 162640-98-4 | SDF | Download SDF |
Synonyms | N/A | ||
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=C35 | ||
Formula | C25H27N5 | M.Wt | 397.52 |
Solubility | Soluble in DMSO | Storage | Store at -20°C |
Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
PGD24 is a lipid mediator involved in sleep and inflammatory responses. PGD2 activates two different types of receptors. PGD2 regulates sleep and pain via DP1 receptors in the central nervous system. This prostanoid also causes contraction of airway smooth muscle via DP1 receptors and mediates chemotaxis of eosinophils and basophils into the lung via DP2 receptors in the periphery. Therefore, PGD2 coordinately regulates allergic reactions, especially airway inflammation, via these two receptors. AT-56 is an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase.
In vitro: AT-56 inhibited human and mouse L-PGDSs in a concentration (3-250 μM)-dependently but did not affect the activities of hematopoietic PGD synthase (H-PGDS), cyclooxygenase-1 and -2, and microsomal PGE synthase-1. AT-56 inhibited L-PGDS activity in a competitive manner against the substrate PGH2 (Km=14 μM) with a Ki value of 75 μM but did not inhibit the binding of 13-cis-retinoic acid, a nonsubstrate lipophilic ligand, to L-PGDS. [2].
In vivo: Orally administered AT-56 (
Clinical trial: Up to now, AT-56 is still in the preclinical development stage.
Reference:[1] Daisuke Irikura, Kosuke Aritake, Nanae Nagata, Toshihiko Maruyama, Shigeru Shimamoto, and Yoshihiro Urade. 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.