AT-56

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AT56 是前列腺素 D2 合酶酶活性的特异性抑制剂，可减弱醛固酮的脂肪形成作用。

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

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.

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 injuryDosage: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.).

AT-56 | AT 56 | AT56

Others

Other Targets

L-PGDS

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162640-98-4

397.52

C25H27N5

>98% (HPLC)

DMSO: > 10 mM

N1(CCCCC2=NNN=N2)CC/C(CC1)=C3C4=CC=CC=C4C=CC5=CC=CC=C/35

4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-piperidine

(-20℃)

With Ice Pack

≥ 2 years