α4β1 antagonist-1

α4β1antagonist-1 (Compound 4) is a highly selective α4β1 integrin antagonist with an IC50 of 15 nM. It inhibits integrin-mediated cell adhesion and the activation of the ERK1/2 signaling pathway. α4β1antagonist-1 also exhibits partial agonist activity on αMβ2 integrin with an EC50 of 23 nM. This compound shows potential for research in chronic inflammatory diseases such as rheumatoid arthritis and multiple sclerosis, as well as in cancer.

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor (hydrochloride).

Dopamine D4 receptor antagonist-1 can be used in schizophrenia study. Dopamine D4 receptor antagonist-1 is a selective antagonist of Dopamine D4 receptor (DRD4). The Ki value of Dopamine D4 receptor antagonist-1 for Hd4.2 is 9.0 nM [1].

D4R Antagonist-1, characterized by its potent and selective antagonistic action against D4 receptors with an IC50 value of 6.87 μM, holds potential for Parkinson's disease research [1].

R-BC154 acetate, a selective fluorescent antagonist of α9β1 integrin, serves as a high-affinity, activation-dependent probe for investigating α9β1 and α4β1 integrin binding activity. This compound is particularly useful for detailed studies on integrin interactions [1].

Compound 11, an α4 integrin receptor antagonist, exhibits oral activity and functions as an antagonist of the α4 integrin receptor. It efficiently inhibits the adhesion of K562 cells mediated by the interactions of α4β1/VCAM-1 and α4β7/MAdCAM-1, with IC50 values of 130 nM and 2 nM, respectively. Compound 11 also shows potential for use in studies using the DSS (dextran sulfate sodium) induced colitis mouse model.