UR-12947 is a platelet glycoprotein (GP) IIb-IIIa antagonist. UR-12947 exhibits potent inhibitory activity against platelet aggregation in human platelet-rich plasma, with an IC50 value of 3.5 nM. UR-12947 can be used in the research of arterial thrombotic diseases.

CP-664511 is an orally active and potent α4β1 integrin antagonist with anti-inflammatory effects (IC50=0.52 nM). CP-664511 inhibits the interaction between α4β1 and vascular cell adhesion molecule-1 (VCAM-1), significantly reducing eosinophil infiltration into lung tissue. CP-664511 is promising for research of asthma and allergic airway diseases.

EMD527040 (hydrochloride) is a highly potent and selective αvβ6 antagonist with anti-fibrotic activity. EMD527040 (hydrochloride) is used in the research of liver cancer and liver fibrosis.

FR-158999 is a potent orally active fibrinogen inhibitor. FR-158999 exhibits potent anti-platelet activities with a pIC50 of 7.50. FR-158999 can be used for antithrombotic research.

ZD 2486 is a glycoprotein IIb/IIIa (GP IIb/IIIa) antagonist. ZD 2486 inhibits platelet aggregation by blocking the binding of fibrinogen to the GP IIb/IIIa receptor on platelets. ZD 2486 can be used for the study of conditions related to unwanted platelet aggregation, such as acute coronary syndrome, unstable angina pectoris, acute myocardial infarction, and complications from cardiovascular interventional procedures[1]

NOTA-IMB-RGD is a dual molecular probe targeting integrin αvβ3 and programmed death ligand-1 (PD-L1). NOTA-IMB-RGD blocks the PD-1/PD-L1 signaling pathway and integrin αvβ3-overexpressing tumor vasculature. NOTA-IMB-RGD is promising for research of solid tumors co-expressing PD-L1 and αvβ3 (e.g., glioma, breast cancer).

RGD-DA6 is an αvβ3-targeted ligand. RGD-DA6 consists of RGDfK (an integrin αvβ3-targeted RGD peptide), DOTADG, d-Glu, Lys, AMBA, and IPBA. RGD-DA6 can be radiolabeled as an αvβ3-targeted radioligand and used for high-contrast tumor imaging and enhanced anticancer efficacy.

BTT-3034, a sulfonamide derivative, is an α2β1 integrin inhibitor. BTT-3034 inhibits cell adhesion to rat tail collagen I with an EC50 of 160 nM and a corresponding Emaxof 86%. BTT-3034 inhibits collagen binding by an α2 variant carrying the conformationally activating E318W mutation.

ME-3277 is a potent GPIIb/IIIa antagonist. ME-3277 reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery (MCA). ME-3277 can be used for the acute cerebral infarction research.

GP1 precursor has high affinity to GPIIb/IIIa receptors of activated platelets. GP1 precursor can be radiolabeled with [18F] and used as a PET Tracer for visualizing active platelet aggregation at the molecular level. GP1 precursor can be used for the detection of Thrombi.

XV459 is an orally active platelet GPIIb/IIIa receptor antagonist. XV459 blocks all agonist induced platelet aggregation by binding to platelet GPIIb/IIIa receptors. XV459 can significantly prolong occlusion time, reduce thrombus weight, and maintain blood flow. XV459 can be used for anti thrombotic research.

CLT-28643 is an integrin α5β1 inhibitor. CLT-28643 can inhibit the high expression of integrin α5β1 in the bleb at early time-points after surgery and promote wound healing process.

Emvistegrast is a quinolone derivative. Emvistegrast is an antagonist of α4β7 integrin. Emvistegrast can be studied in research for diseases that are mediated by α4β7 integrin, such as infkammatory bowel disease.

NPC-15669 is a novel Mac-1 inhibitor. NPC-15669 reduces plasma levels of ET-1, TxB, prostacyclin, AT-III, and total protein S. NPC-15669 can be used in the research of myocardial infarction.

BIRT2584 is an LFA-1 inhibitor. BIRT2584 can be used for research on autoimmune diseases.

L-767685, the ethyl ester prodrug of L-767679), is a non-peptide glycoprotein IIb/IIIa receptor (GPIIb-IIIa receptor) antagonist. L-767679 has a potent anti-platelet aggregation effect. L-767685 can be used for research on antithrombosis.

K34c hydrochloride is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c hydrochloride reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c hydrochloride can be used in glioblastoma research.

EMD-132338 is a GPIIb/IIIa (αIIbβ3) antagonist that inhibits platelet aggregation. EMD-132338 can be utilized in antithrombosis research.

Des-ethyl-carafiban (Compound 44) is a fibrinogen receptor antagonist that can effectively inhibit platelet aggregation induced by multiple agonists. Des-ethyl-carafiban can be used in the research of thrombotic diseases.

Carotegrast methyl (AJM300) hydrochloride is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl hydrochloride, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl hydrochloride prevents the development of colitis in mice.

​​THI0019​​ represents a novel class of integrin modulators with unique agonist activity targeting multiple adhesion receptors.

GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media.

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

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

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.

TBC 4746 (AVA4746) is a small molecule mimetic of VCAM-1 that binds VLA-4 on B-ALL cells with high affinity and efficiently blocks ligand-binding with VCAM-1 with EC50 of 38.52 nM.

MSR03 is a potent, pure small molecule αVβ3 antagonist with IC50 of 1.5 uM for inhibition of adhesion of cells expressing human αVβ3 to immobilized fibrinogen.

IVL745 (IVL-745) is a small molecule very late antigen (VLA-4) antagonist with IC50 of 20 nM and 2 nM for adhesion to VCAM-1 and fibronectin, respectively.

GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively.