Carotegrast methyl

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].
In Vitro: HCA2969 inhibits human α4β1 integrin (K_D=0.32 nM; IC₅₀=5.8 nM), human α4β7 integrin (K_D=0.46 nM; IC₅₀=1.4 nM) and mouse α4β7 integrin (K_D=0.2 nM; IC₅₀=26 nM) in Jurkat, RPMI-8866 and TK-1 cell lines^[1]. In Vivo: 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].