α4β7 Inhibitor

BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (K_d<10 pM). BIO5192 selectively binds to α4β1 (IC₅₀=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

Etrolizumab (rhuMAb Beta7) is a gut-selective, anti-β7 integrin monoclonal antibody. Etrolizumab is specific targeting of the β7 subunit of α4β7 and αEβ7 integrins with K_i values of 18 nM and 1800 pM for Human α4β7 and Human αEβ7-293, respectively. Etrolizumab can be used in research of inflammatory bowel disease (IBD).

BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC₅₀ values of 4 nM and 2 μM for α4β1 and α4β7, respectively.

α4β7 Integrin-IN-2 is an inhibitor of human α4β7 integrin with an IC₅₀ <5 nM. α4β7 Integrin-IN-2 modulates α4β7 integrin-mediated biological pathways. α4β7 Integrin-IN-2 can be used for the research of inflammatory dieases.

Deethyl-emvistegrast is a quinoline derivative and also a α4β7 integrin inhibitor. Deethyl-emvistegrast is the hydrolytic product of Emvistegrast (HY-177080). Deethyl-emvistegrast modulates inflammatory pathways. Deethyl-emvistegrast can be used in research related to inflammatory bowel disease (Crohn's disease and ulcerative colitis).

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (K_d<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC₅₀=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

α4β7 Integrin-IN-1 (Example 356) is a potent inhibitor of α4β7 integrin (integrin). Its ability to block the interaction between α4β7 integrin and MadCAM-1 (EC₅₀) is 0.05 nM. α4β7 Integrin-IN-1 can be used for the study of inflammatory bowel disease.

α4 integrin receptor antagonist 3 (Compound 11) is an orally active α₄integrin receptor antagonist. α4 integrin receptor antagonist 3 can inhibit the adhesion of K562 cells mediated by the interaction between α₄β₁/VCAM-1 and α₄β₇/MAdCAM-1, with IC₅₀ values of 130 nM and 2 nM, respectively. α4 integrin receptor antagonist 3 has the potential to be used in the study of dextran sulfate sodium (DSS) colitis mouse model.

(S)-Deethyl-emvistegrast is the S-enantiomer of Deethyl-emvistegrast (HY-186079). Deethyl-emvistegrast is a quinoline derivative and also a α4β7 integrin inhibitor. It acts as the hydrolysis product of Emvistegrast (HY-177080). Deethyl-emvistegrast modulates inflammatory pathways and can be used in research related to inflammatory bowel diseases (Crohn's disease and ulcerative colitis).