Integrin Inhibitor

(R/S)-Alicaforsen is the racemate of Alicaforsen composed of R and S configurations. Alicaforsen is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation.

XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo.

Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) (Cyclo(RGDfV) (TFA))is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) can be used for the research of acute myeloid leukemia.

BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC₅₀ of 2.5 nM in the adhesion assay and an IC₅₀ of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model.

Zaurategrast (CT7758) is a potent and oral-effective α₄-integrin inhibitor.

LDV is a non-fluorescent analog of LDV-FITC. LDV is a α4β1 integrin (VLA-4) ligand, and binds α4β1 integrin in leukemia cells.

LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC₅₀ of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.

Integrin signaling inhibitor, mP13 is an inhibitor of integrin signaling. Integrin signaling inhibitor, mP13 inhibits inside-out and outside-in signaling, including fibrinogen binding, platelet adhesion, and clot retraction.

Vatelizumab (GBR500) is a monoclonal antibody that targets the α2 subunit (CD49b) of very late antigen 2 (VLA-2). Vatelizumab can be used for research on multiple sclerosis.

Elsibucol is a VCAM1 inhibitor for the study of organ transplant rejection. Elsibucol is a metabolically stable propanol derivative with antioxidant, anti-inflammatory and anti-proliferative properties. Elsibucol lowers blood cholesterol levels and reduces oxidative stress and inflammatory responses in injured arteries, thereby inhibiting atherosclerosis and protecting endothelial healing after arterial injury.

GRGDSP (TFA) is an integrin inhibitor.

Risuteganib hydrochloride is a synthetic RGD (arginyl-glycyl-aspartic acid)-class peptide. Risuteganib hydrochloride is an anti-integrin that downregulates oxidative stress and restores homeostasis, and targets three integrin receptors that are implicated in dry age-related macular degeneration (AMD) in order to restore homeostasis in the retina.

G-Pen-GRGDSPCA TFA is an αvβ3-inhibiting RGD peptide. G-Pen-GRGDSPCA can limit neointimal hyperplasia and lumen stenosis after vascular injury, as well as regulate the migration and proliferation of smooth muscle cells. G-Pen-GRGDSPCA TFA can be used in the study of the mechanism of vascular injury repair.

LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC₅₀ of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.

Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC₅₀ values of 7.8, 8.4, 8.4 and 7.4, respectively.

Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research .

Rondaptivon pegol (BT200) is a pegylated aptamer targeting von Willebrand factor (VWF), with an EC₅₀ of 33 nM in humans. Rondaptivon pegol effectively alleviates acute myocardial ischemia-reperfusion injury in mice by inhibiting VWF activity, reducing microvascular obstruction, inflammatory responses and cardiomyocyte apoptosis (apoptosis). Rondaptivon pegol inhibits the binding of VWF to platelet glycoprotein GPIb, thereby preventing arterial thrombosis in cynomolgus monkeys. Rondaptivon pegol can be used in research related to arterial thrombosis, stroke, myocardial infarction and myocardial ischemia-reperfusion injury.

Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke.

αVβ8-IN-1 is a αVβ8 integrin inhibitor. αVβ8-IN-1 has been shown to inhibit the growth of tumors such as EMT6, CT26, KPC, and TKCC-10. αVβ8-IN-1 can be used in research related to idiopathic pulmonary fibrosis (IPF), non-specific interstitial pneumonia (NSIP), and tumors.

FITC-Ahx Gly Arg Gly Asp Ser Pro is a GRGDSP (HY-P0290) coupled to FITC. GRGDSP is an integrin inhibitor that can inhibit the adherence of tumor cells to endothelial cells of blood vessels and limit its metastasis.