integrin α4β1

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.

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.

Natalizumab is a recombinant humanized monoclonal antibody and a humanized monoclonal antibody inhibitor that selectively targets α4 integrin (CD49d). Natalizumab binds to the α4β1 heterodimer and blocks its interaction with vascular cell adhesion molecule 1. Natalizumab also prevents lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses, and is used in the study of relapsing-remitting multiple sclerosis and Crohn’s disease. Natalizumab possesses anti-inflammatory and immunomodulatory activity, inhibiting the adhesion, retention, and transendothelial migration of immune cells, and reducing the infiltration of inflammatory cells into the central nervous system or affected sites. Natalizumab is also being studied for autoimmune or inflammation-related diseases such as B-cell lymphoma and non-infectious uveitis.

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.

TCS 2314 (compound 3) is a potent and selective VLA-4 (α4β1 integrin; CD49d/CD29) antagonist with an IC50 of 4.4 nM. It exhibits high plasma clearance and low oral bioavailability in rats, making it suitable for asthma research.

RO0505376 is an α4β1 integrin antagonist.

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.

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.

BIO-1211 is a more potent inhibitor of α4β1 (VLA-4, IC50 = 4 nM) over α4β7(IC50 = 2 μM).

fluorescent ligand that binds to the α4β1 integrin (VLA-4)

BIO-7662 is an effective and highly selective antagonist of α4β1 integrin.

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.

Integrin modulator 1 is a potent and selective α4β1 integrin agonist with an IC50 value of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 enhances cell adhesion mediated by α4β1 integrin with an EC50 of 12.9 nM, highlighting its utility in studying integrin-dependent adhesion processes.

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd < 10 pM). The compound selectively binds to α4β1 (IC50 = 1.8 nM) over various other integrins and results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

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.

BOP-JF549 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor® 549. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 549 nm; emission maximum = 571 nm.

BOP-JF646 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor®646. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 655 nm; emission maximum = 672 nm.