2. シグナル伝達
  3. Cytoskeleton
  4. Integrin
  5. α4β1 Isoform

α4β1

α4β1 integrin (very late antigen-4, VLA-4) is a heterodimeric adhesion receptor that regulates leukocyte trafficking, cell adhesion, and immune cell communication through interactions with vascular cell adhesion molecule-1 (VCAM-1), fibronectin, and related ligands[4][5]. Mechanistically, α4β1 plays a central role in leukocyte tethering, rolling, firm adhesion, and transendothelial migration during inflammatory responses, thereby controlling immune-cell recruitment to inflamed tissues[4][5]. Through α4β1-VCAM-1 signaling, activated lymphocytes and monocytes gain access to target organs, linking this integrin directly to inflammatory and autoimmune disease pathogenesis[4][1]. In disease models, α4β1 is required for T-cell migration across the blood-brain barrier, and blockade of α4-mediated adhesion suppresses experimental autoimmune encephalomyelitis, supporting its relevance to multiple sclerosis and related neuroinflammatory disorders[4]. α4β1 also contributes to leukocyte accumulation in chronic inflammatory conditions, making it a validated therapeutic target in immune-mediated diseases[4][1][2]. Compared with the related α4β7 integrin, which preferentially mediates lymphocyte homing to intestinal tissues through interactions with mucosal addressin cell adhesion molecule-1 (MAdCAM-1), α4β1 primarily mediates adhesion to VCAM-1 and functions broadly in systemic inflammatory trafficking[3]. This distinction is important for experimental design because α4β1 and α4β7 exhibit overlapping yet biologically distinct ligand-recognition and tissue-homing properties[3]. For research applications, selective α4β1 antagonists and inhibitory antibodies are widely used to investigate leukocyte migration pathways, whereas highly selective small-molecule inhibitors such as BIO5192 provide experimental tools for dissecting α4β1-dependent adhesion mechanisms with minimal activity toward other integrins[2].

α4β1 関連製品 (21):

製品番号 製品名 製品効果 純度
  • HY-108831
    Natalizumab Inhibitor 99.10%
    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.
  • HY-107589
    BIO5192 Inhibitor 99.96%
    BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<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.
  • HY-134130
    Integrin modulator 1 Agonist 99.80%
    Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
  • HY-15770
    TR-14035 Antagonist 99.87%
    TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.
  • HY-14951
    Firategrast Antagonist 99.75%
    Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
  • HY-171216
    GW559090 Antagonist
    GW559090 is a selective, competitive, and high-affinity α4 integrin antagonist with a Kd of 0.19 nM for α4β1. GW559090 can effectively block the binding of α4β1 to vascular cell adhesion molecule 1 (VCAM-1) and fibronectin with IC50 values of 7.72 and 8.04 nM. GW559090 also inhibits the interaction between α4β7 and mucosal addressin cell adhesion molecule 1 (MAdCAM-1) (IC50 = 23 nM). GW559090 can inhibit inflammatory infiltration in the eyes, repair the corneal barrier and restore the function of goblet cells. GW559090 can be used for research of Sjögren's syndrome associated dry eye.
  • HY-14126
    BIO-1211 Inhibitor 99.64%
    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.
  • HY-107589A
    BIO5192 hydrate Inhibitor 99.96%
    BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<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.
  • HY-139702
    α5β1 integrin agonist-1 Agonist 99.67%
    α5β1 integrin agonist-1 is an α5β1 integrin agonist, with an EC50 of 1.5 nM. α5β1 integrin agonist-1 inhabits α4β1 integrin (IC50 = 2.99 μM) in Jurkat/VCAM-1 adhesion assayα5β1 integrin agonist-1 induces concentration-dependent apoptosis and activates the caspase 3/7 pathway in α5β1 integrin-expressing K562 cancer cells. α5β1 integrin agonist-1 can be used for the study of cancer.
  • HY-129453
    BOP sodium Inhibitor 99.25%
    BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd 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.
  • HY-P990144
    Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) Inhibitor
    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.
  • HY-138542
    RO0270608 Antagonist 98.80%
    RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity.
  • HY-P11445
    GREDVGC 99.45%
    GREDVGC is a peptide. GREDVGC can mimic VCAM-1 for binding to integrin α4β1. GREDVGC can be used for the research of cancer.
  • HY-175286
    α4β1 antagonist-1 Antagonist
    α4β1 antagonist-1 (Compound 4) is a highly selective α4β1 integrin antagonist (IC50=15 nM). α4β1 antagonist-1 inhibits integrin-mediated cell adhesion and ERK1/2 signaling activation. α4β1 antagonist-1 also exhibits partial agonism toward αMβ2 integrin (EC50=23 nM). α4β1 antagonist-1 is promising for research of chronic inflammatory diseases (e.g., rheumatoid arthritis, multiple sclerosis) and cancers.
  • HY-114225
    TBC-4746 Antagonist
    TBC-4746 is a α4β1/α4β7 integrin antagonist. TBC-4746 can be used in the research of asthma and multiple sclerosis.
  • HY-14277
    Levocabastine Antagonist
    Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).
  • HY-159179
    α4 integrin receptor antagonist 3 Inhibitor
    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.
  • HY-119142
    CP-664511 Antagonist
    CP-664511 is an orally active and potent α4β1 integrin antagonist with anti-inflammatory effects (IC50=0.52 nM). CP-664511 inhibits the interaction between α4β1 and vascular cell adhesion molecule-1 (VCAM-1), significantly reducing eosinophil infiltration into lung tissue. CP-664511 is promising for research of asthma and allergic airway diseases.
  • HY-123164
    IVL 745 Antagonist
    IVL 745 (XRP 1745A) is a very late antigen 4 (VLA-4, integrin α4β1) antagonist. IVL 745 reduces the airway inflammatory response of sensitized rats and sheep. IVL 745 can be used for airway inflammation and asthma research.
  • HY-14189
    Valategrast hydrochloride Antagonist
    Valategrast hydrochloride (R-411) is a potent integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast hydrochloride has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.