AT-56

SKU: orb1226031

Description

AT56, a specific inhibitor of prostaglandin D2 synthase enzymatic activity, blunted adipogenic aldosterone effects.

Key Properties

• CAS Number: 162640-98-4
• MW: 397.52
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₇N₅
• SMILES: N1(CCCCC2=NNN=N2)CC/C(CC1)=C3C4=CC=CC=C4C=CC5=CC=CC=C/35
• Target: L-PGDS
• Solubility: DMSO: > 10 mM

Bioactivity

• In Vivo:
  AT-56 (1-30 mg/kg; p.o.) suppresses the PGD2 production in the stab-wounded brain. AT-56 (1-10 mg/kg; p.o.) suppresses the L-PGDS-mediated allergic airway inflammation in mice. AT-56 (10 mg/kg; p.o.) exhibits Cmax (2.15 μg/ml), half-life (1.71 h) and high oral bioavailability (82%). Animal model: H-PGDS KO mice (14-16weeks, 25-30 g, C57BL/6 strain) with a stab wound brain injury. 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). 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). 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.).
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AT-56 | AT 56 | AT56

Quick Database Links

Gene Symbol

L-PGDS