α4β1 integrin

Natalizumab used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease.

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

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.

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.

RO0505376 is an α4β1 integrin antagonist.

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.

Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1, and increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM[1].

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.

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

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

ProMMP-9 inhibitor-3c is a potent and specific proMMP-9 inhibitor which disrupts f MMP-9 homodimerization and prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR.

R-BC154 acetate, a selective fluorescent antagonist of α9β1 integrin, serves as a high-affinity, activation-dependent probe for investigating α9β1 and α4β1 integrin binding activity. This compound is particularly useful for detailed studies on integrin interactions [1].

REDV is a minimal active sequence found in the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin, critical for mediating adhesion to the IIICS region of plasma fibronectin through binding with integrin alpha 4 beta 1 (α4β1). It is utilized in cell adhesion research [1].

REDV TFA, the minimal active sequence of the CS5 site in the alternatively spliced type III connecting segment (IIICS) of fibronectin, mediates adhesion to the IIICS region of plasma fibronectin through binding with the integrin alpha 4 beta 1 (α4β1). It is utilized in cell adhesion research [1].