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AM211(AM211 free acid)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AM211(AM211 free acid)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
AM211 (AM211 free acid) 是一种有效的、选择性的、口服生物可利用的前列腺素 D2 (PGD2) 受体 2 (DP2) 拮抗剂,对人、小鼠、豚鼠和豚鼠的 IC50 分别为 4.9 nM、7.8 nM、4.9 nM、10.4 nM 和大鼠 DP2,分别。

Animal experiment:

Mice[1]In brief, mice are immunized by an intraperitoneal injection of 10 μg of ovalbumin (OVA) complexed with Imject Alum in a volume of 0.2 mL on days 1 and 8. Seven days later (day 15) mice are challenged intranasally with 20 μL of a 10 mg/mL solution of OVA. The challenge period occurs daily from days 15 to 19. Mice (seven/group) are randomLy assigned to receive either compound (AM211, 10 mg/kg) or vehicle (methyl cellulose, 10 mL/kg) and treated by oral gavage 1 h before each OVA challenge. The number of sneezes are counted for 8 min immediately after the OVA challenge on days 15, 17, and 19 by an independent observer who is blinded to the treatment groups[1].

产品描述

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.

AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 displays high selectivity for DP2 versus other receptors in the prostanoid family, with IC50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP of more than 100 μM. AM211 (100 μM) shows no activity at COX-1, COX-2 enzymes as well as PPAR family of nuclear receptors[1].

AM211 (1, 10, and 30 mg/kg, p.o.) dose-dependently decreases in the number of DK-PGD2-induced peripheral blood leukocytes, with a calculated ED50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced pulmonary inflammation in guinea pigs. AM211 (10 mg/kg, p.o.) causes significant decrease in ovalbumin (OVA)-induced sneezing in a mouse model of allergic rhinitis[1].

[1]. Bain G, et al. Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation. J Pharmacol Exp Ther. 2011 Jul;338(1):290-301.