α4β1 Inhibitor

Natalizumab (AN100226; BG00002) is a humanized monoclonal IgG4 antibody inhibitor that selectively targets α4 integrin (CD49d). It blocks the interaction of integrins such as α4β1 (VLA-4) with vascular cell adhesion molecule VCAM-1, intercellular adhesion molecule ICAM-1, and fibronectin by competitively binding to the α4 subunit. Natalizumab inhibits the adhesion, retention, and transendothelial migration of immune cells (such as CD4⁺ T cells), reducing the infiltration of inflammatory cells into the central nervous system or lesion sites, thus exerting anti-inflammatory and immunomodulatory activity. Natalizumab is used in the study of relapsing-remitting multiple sclerosis (RRMS) and also has applications in the study of autoimmune or inflammation-related diseases such as Crohn's disease, B-cell lymphoma, and non-infectious uveitis. Natalizumab can also prevent lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses.

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.

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.

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.

BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with K_d values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.

Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) is an anti-mouse/human VLA-4/CD49d IgG2b monoclonal antibody. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can reduce VLA-4 positive cells. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can inhibit the migration of Tc1 cells to tumors. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) inhibits the retention of leukemia cells in the spleen and bone marrow by blocking VLA-4. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can be used for research on inflammation conditions and cancer such as experimental autoimmune encephalomyelitis (EAE), melanoma and leukemia.

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.

HMR 1031 is a very late antigen-4 (VLA4, i.e., integrin α4β1) inhibitor, with IC₅₀ values of 0.7 nM and 0.3 nM against VLA-4/VCAM-1 and VLA-4/fibronectin, respectively. HMR 1031 blocks allergen-induced airway responses and airway inflammation in mouse and sheep models. HMR 1031 can be used in asthma-related research.