|S7077||Cilengitide trifluoroacetate||8 mg/mL||100 mg/mL||<1 mg/mL|
|S8008||RGD (Arg-Gly-Asp) Peptides||12 mg/mL||<1 mg/mL||<1 mg/mL|
|S2885||A-205804||<1 mg/mL||60 mg/mL||<1 mg/mL|
|S3085||Tirofiban||<1 mg/mL||0.005 mg/mL||<1 mg/mL|
|S7540||SB273005||<1 mg/mL||90 mg/mL||16 mg/mL|
|S3714||Lifitegrast||<1 mg/mL||100 mg/mL||20 mg/mL|
|S8454||ATN-161 (Ac-PHSCN-NH2)||13 mg/mL||-1 mg/mL||-1 mg/mL|
|S8594||Tirofiban Hydrochloride||95 mg/mL||95 mg/mL||95 mg/mL|
|S7834||Cyclo (-RGDfK)||84 mg/mL||100 mg/mL||<1 mg/mL|
|S8306||Leukadherin-1||<1 mg/mL||15 mg/mL||<1 mg/mL|
|S7844||Cyclo(RGDyK)||100 mg/mL||100 mg/mL||20 mg/mL|
Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.
WT mice were subjected to BDL and treated with either vehicle or cilengitide (10 mg/kg) daily for 6 days; adjacent liver sections were immunostained for CK19 or PCNA. Data were quantified and expressed as mean ± SD. (n = 6 per group.) *P < 0.02, **P < 0.004, Student’s t test.
RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins.
BC, aMPV/B F protein fusogenic activity was determined using syncytium formation and reporter gene assays. RGE peptides (80 μM) were used as the control.
A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively.
MDA-MB-231 cells transfected with ICAM-1-specific siRNAs or treated for 12 h with A-205804 at the indicated concentrations were subjected to immunoblotting with indicated antibodies. Densitometric data (fold) were shown below each group.
Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.
SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
Lifitegrast is a novel small molecule integrin antagonist that inhibits a specific T cell-mediated inflammatory pathway involved in the pathogenesis of DED.
ATN-161 (Ac-PHSCN-NH2) is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
Tirofiban Hydrochloride is the hydrochloride salt form of tirofiban, a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation. It is more soluable than Tirofiban.
Cyclo (-RGDfK) is a potent and selective αvβ3 integrin inhibitor.
Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)).
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.