AT-56 - CAS:162640-98-4

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AT-56

目录号 : KM11563 CAS No. : 162640-98-4 纯度 : ≥98%

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AT-56 是一种有效，选择性和具有口服活性的脂钙蛋白型前列腺素 D 合酶 (L-PGDS) 的抑制剂，IC₅₀ 值为 95 μM，K_i 值为 75 μM。AT-56 可选择性抑制 L-PGDS 催化的 PGD₂ 介导的嗜睡或疼痛反应。

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生物活性

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 K_i of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD₂.

体外研究

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.

体内研究

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 C_max (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%); C_max (2.15 μg/ml); T_1/2 (1.71 h, p.o.); T_1/2 (2.35 h, i.v.).

分子式

C₂₅H₂₇N₅

分子量

397.52

CAS号

162640-98-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

纯度： ≥98%

Data Sheet

产品使用指南

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