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AT 56

Catalog No.GC11950

L-PGDS inhibitor

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AT 56 Chemical Structure

Cas No.: 162640-98-4

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5mg
$55.00
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10mg
$83.00
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50mg
$381.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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 (<30 mg/kg body weight) decreased the PGD2 production to 40% in the H-PGDS-deficient mice brain after a stab wound injury in a dose-dependent manner without affecting the production of PGE2 and PGF2α and also suppressed the accumulation of eosinophils and monocytes in the bronco-alveolar lavage fluid from the antigen-induced lung inflammation model of human L-PGDS-transgenic mice [3].

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.

Chemical Properties

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.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.5156 mL 12.578 mL 25.156 mL
5 mM 0.5031 mL 2.5156 mL 5.0312 mL
10 mM 0.2516 mL 1.2578 mL 2.5156 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 19 reference(s) in Google Scholar.)

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