α4 integrin receptor

Carotegrast, an orally available α4 integrin receptor inhibitor, has anti-inflammatories activities.

α4integrinreceptor antagonist 3(Compound 11)是一种口服活性的α4整合素受体拮抗剂.该化合物能有效抑制 K562 细胞通过α4β1 VCAM-1和α4β7 MAdCAM-1相互作用的粘附,其IC50值分别为 130 nM 和 2 nM.此外,α4integrinreceptor antagonist 3 在葡聚糖硫酸钠(DSS)诱导的结肠炎小鼠模型中显示了研究潜力.

Carotegrast methyl (AJM300) 是一种口服有效和选择性 α4 整联蛋白拮抗剂，可预防小鼠结肠炎。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, also known as AJM300 and PTC-100, is an orally-active small molecule that antagonises the α4 integrin receptor. AJM300 reduces inflammation by blocking leucocyte trafficking. Oral treatment with AJM300 dose-dependently inhibited lymphocyte homing to Peyer's patches and increased the peripheral lymphocyte count in the same dose range. AJM300 dose-dependently prevented the development of experimental colitis in mice.