AT-56

Modify Date: 2024-01-02 11:04:54

AT-56 Structure
AT-56 structure
Common Name AT-56
CAS Number 162640-98-4 Molecular Weight 397.515
Density 1.2±0.1 g/cm3 Boiling Point 620.4±65.0 °C at 760 mmHg
Molecular Formula C25H27N5 Melting Point N/A
MSDS Chinese USA Flash Point 329.0±34.3 °C

 Use of AT-56


AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2[1].

 Names

Name 4-(dibenzo[1,2-a:1',2'-e][7]annulen-11-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]piperidine
Synonym More Synonyms

 AT-56 Biological Activity

Description AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2[1].
Related Catalog
Target

IC50: 95 μM (L-PGDS); Ki: 75 μM (L-PGDS)[1]

In Vitro AT-56 (1-30 μM; 10 minutes) dose-dependently inhibits the production of PGD2 in L-PGDS-expressing human medulloblastoma TE-671 cells with an IC50 of about 3 μM[1].
In Vivo AT-56 ( 1-30 mg/kg; p.o.) suppresses the PGD2 production in the stab-wounded brain[1]. AT-56 (1-10 mg/kg; p.o.) suppresses the L-PGDS-mediated allergic airway inflammation in mice[1]. AT-56 (10 mg/kg; p.o.) exhibits Cmax (2.15 μg/ml), half-life (1.71 h) and high oral bioavailability (82%)[1]. Animal Model: H-PGDS KO mice (14-16weeks, 25-30 g, C57BL/6 strain) with a stab wound brain injury[1] Dosage: 0, 1, 3, 10, 30 mg/kg Administration: P.o. 1 h before the stab wound injury Result: Inhibited the L-PGDS reaction in the brain. Decreased the total amount of PGD2 in the brain to 40% with 30 mg/kg AT-56. Animal Model: Human L-PGDS-overexpressing TG mice (males, 14-16 weeks, 25-30 g)[1] Dosage:  0, 1, 10 mg/kg Administration: P.o. 1 h before and 24 h after the antigen exposure Result: Prevented the eosinophil infiltration by inhibiting transgened human L-PGDS. Animal Model: Male C57BL/6 mice (7 weeks, 22-26 g)[1] Dosage: 10 mg/kg for p.o. and 2 mg/kg for i.v. (Pharmacokinetic Analysis) Administration: P.o. and i.v. administration Result: Oral bioavailability (82%); Cmax (2.15 μg/ml); T1/2 (1.71 h, p.o.); T1/2 (2.35 h, i.v.).
References

[1]. Irikura D, et, al. 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 & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 620.4±65.0 °C at 760 mmHg
Molecular Formula C25H27N5
Molecular Weight 397.515
Flash Point 329.0±34.3 °C
Exact Mass 397.226654
PSA 57.70000
LogP 5.84
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.646
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-[4-(1H-tetrazol-5-yl)butyl]piperidine
ICI 215,001 hydrochloride
AT-56
Piperidine, 4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: AT-56
  • Price: $550.0/100mg $1000.0/250mg $1600.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


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