Carotegrast methyl (AJM300) 是一种口服有效和选择性 α4 整联蛋白 (α4 integrin) 拮抗剂。HCA2969 是 Carotegrast methyl 的活性代谢产物，是一种特异的双重 α4β1/α4β7 整联蛋白拮抗剂。Carotegrast methyl 可预防小鼠结肠炎。
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice[1].
HCA2969 inhibits human α4β1 integrin (KD=0.32 nM; IC50=5.8 nM), human α4β7 integrin (KD=0.46 nM; IC50=1.4 nM) and mouse α4β7 integrin (KD=0.2 nM; IC50=26 nM) in Jurkat, RPMI-8866 and TK-1 cell lines[1].
Carotegrast methyl (AJM300; oral; 0.03-1%; for 15 days) prevents the development of colitis induced by transfer of IL-10 deficient CD4+ T cells in mice[1]. Carotegrast methyl (oral; 0.3, 3, 30, or 30 mg/kg; a single oral) inhibits Lymphocyte homing to Peyer’s patches and increases peripheral lymphocyte counts in a dose-dependent manner in BALB/c mice (8 weeks of age, female)[1].
[1]. Toshihiko Sugiura, et al. Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice. J Crohns Colitis. 2013 Dec;7(11):e533-42.
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