αIIbβ3 Inhibitor

Cilengitide (EMD 121974) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

Cilengitide TFA (EMD 121974 TFA) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide TFA inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide TFA inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide TFA can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

Tadocizumab (C4G1; YM-337) is a humanized monoclonal antibody tageting integrin αIIbβ3. Tadocizumab has antiplatelet and antithrombotic effects, and can be used for cardiovascular disease research.

αvβ5 integrin-IN-3 is an orally active, selective αVβ5 integrin inhibitor with an IC₅₀ value of 0.61 nM. αvβ5 integrin-IN-3 inhibits αVβ1, αVβ3 and αVβ6 integrins with IC₅₀ values of 21 nM, 5.5 nM and 18 nM, respectively. αvβ5 integrin-IN-3 reduces total Collagen content in a mouse unilateral ureteral obstruction model. αvβ5 integrin-IN-3 can be used for the research of renal fibrosis.

IP/EP4 receptor agonist-1 is a PGI₂ analog and also an IP/EP4 receptor agonist. IP/EP4 receptor agonist-1 inhibits PAR-mediated integrin α_IIbβ₃ activation, P-selectin exposure, platelet aggregation and thrombus formation. IP/EP4 receptor agonist-1 can be used in research related to pulmonary hypertension.

Cilengitide hydrochloride (EMD 121974 hydrochloride) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC₅₀ values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide hydrochloride inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide hydrochloride inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide hydrochloride can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.

Ro 44-3888 is an orally active and selective GP IIb-IIIa (fibrinogen receptor, integrin α_IIbβ₃) inhibitor with an IC₅₀ of 1.9 nM against the human target. Ro 44-3888 blocks the binding of fibrinogen to GP IIb-IIIa and inhibits human ADP-induced platelet aggregation. Ro 44‑3888 is formed via the metabolism of the double prodrug Ro 48‑3657 (HY-10309). Ro 44-3888 is used in studies related to arterial thrombosis.