α4β7 integrin

RO0270608, the active metabolite of R411, is an orally active dual α4β1/α4β7 integrin antagonist with anti-inflammatory properties, useful for studying allergic inflammatory responses.

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).

α4β7Integrin-IN-1 (Example 356) is a potent inhibitor of the α4β7 integrin, effectively blocking the interaction between α4β7 integrin and MadCAM-1 with an EC50 of 0.05 nM. This compound is utilized in research related to inflammatory bowel disease.

Anti-Mouse LPAM-1/Integrinα4β7 Antibody (DATK32) is a rat-derived IgG2a, κ antibody inhibitor targeting mouse LPAM-1/Integrinα4β7.

Emvistegrast is a quinolone derivative that acts as an antagonist for the α4β7 integrin.

gp120-α4β7 binding inhibitor 11 is an anti-HIV agent. gp120-α4β7 binding inhibitor 11 interferes the binding of HIV associated glycoprotein gp12G with the integrin α4β7 (IC50=1.64nM).

Valategrast is a potent and orally active dual antagonist of integrin α4β1 (VLA-4) and α4β7, with the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.

Zaurategrast ethyl ester sulfate is a α4β1/α4β7 integrin antagonist, and used for the treatment of inflammatory and autoimmune disorders.

Zaurategrast ethyl ester is the ethyl ester prodrug of CT7758 and is an α4β1/α4β7 integrin antagonist. It is used for the treatment of inflammatory and autoimmune disorders.

Carotegrast is a selective α4 integrin antagonist that inhibits the migration of inflammatory cells to the intestinal mucosa by blocking the interaction between α4β1/α4β7 integrins and their ligands. Carotegrast is used in research and clinical practice for the treatment of inflammatory bowel diseases such as ulcerative colitis; it exerts local anti-inflammatory effects and results in low systemic exposure.

GS-1427 (Emvistegrast) is a quinolone derivative and integrin α4β7 antagonist for studying α4β7 integrin-mediated diseases such as inflammatory bowel disease (IBD).

GW559090 is a selective, competitive, and high-affinity α4 integrin antagonist with a Kd value of 0.19 nM for α4β1. It effectively inhibits the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin, with IC50 values of 7.72 and 8.04 nM, respectively. Additionally, GW559090 suppresses the interaction between α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) with an IC50 value of 23 nM. It also inhibits inflammatory infiltration in the eye, repairs the corneal barrier, and restores goblet cell function, making it useful for research into dry eye syndrome associated with Sjögren's syndrome.

Valategrast hydrochloride (R411), a dual antagonist of integrin α4β1 (VLA-4), is used for the potential treatment of asthma.

Carotegrast methyl (AJM300), an orally-active small molecule, can antagonize the α4 integrin receptor. It is a specific and dual α4β1/α4β7 integrin antagonist.

THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.

TBC-3486 is a novel potent inhibitor of integrin α4, being 200-fold more potent in inhibiting α4β1 than α4β7.

Abrilumab (MEDI-7183) is a fully human monoclonal antibody against α4β7 that inhibits the α4β7 integrin and can be used to study inflammatory bowel disease and ulcerative colitis.

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.

Vedolizumab, a humanized monoclonal antibody, targets the α4β7 integrin for treating Crohn's disease and ulcerative colitis.

Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitum