Arg-Gly-Asp-Ser(RGDS peptide) is an integrin binding sequence that inhibits integrin receptor function; decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS

BIO1211 (BIO-1211) is a potent, highly specific integrin α4β1 (VLA-4) inhibitor with Kd/IC50 of 20 pM/4 nM for the activated form of α4β1.

CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.

cyclo(-RGDfK,-Arg-Gly-Asp-D-Phe-Lys)) is a selective αvβ3-integrin antagonist.

Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.

DS-70 (α4 integrin inhibitor DS-70) is a novel potent α/β- peptidomimetic antagonist of α4 integrin, binds to integrin α4β1 with nanomolar affinity.

SAR 1118 is a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist for treating dry eye.

Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist

Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist.

Valategrast (R411), a small molecule antagonist of α4β1 integrin, represents a potential therapy for asthma

Zaurategrast(CDP-323) is an oral α4-integrin inhibitor.

GLPG0187 is a small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity.

αvβ1 integrin-IN-1 (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. Antifibrotic effects.

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.

c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.

α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

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.

Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.

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.

ILK-IN-3 is an integrin linked kinase inhibitor with antitumor activity.

THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.

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.