Integrin Antagonist

Integrin Antagonists (71):

Cat. No.	Product Name	Effect	Purity

HY-16141

Cilengitide	Antagonist	99.80%
Cilengitide (EMD 121974) is a potent integrins antagonist with IC₅₀s of 0.61 nM (α_νβ₃), 8.4 nM (α_νβ₅) and 14.9 nM (α₅β₁), respectively. Cilengitide inhibits the binding of α_νβ₃ and α_νβ₅ to Vitronectin with IC₅₀s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.

HY-100506

GLPG0187	Antagonist	99.43%
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α_vβ₁-integrin with an IC₅₀ of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.

HY-19344

Lifitegrast	Antagonist	99.29%
Lifitegrast (SAR 1118) is a potent integrin antagonist. Lifitegrast blocks the binding of intercellular adhesion molecule 1 (ICAM-1) to lymphocyte function-associated antigen 1 (LFA-1), interrupting the T cell-mediated inflammatory cycle. Lifitegrast inhibits Jurkat T cell attachment to ICAM-1 with an IC₅₀ of 2.98 nM. Lifitegrast can be used for researching dry eye disease.

HY-15102

MK-0429	Antagonist	99.50%
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC₅₀ values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.

HY-13535A

ATN-161 trifluoroacetate salt	Antagonist	99.04%
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.

HY-P9911

Vedolizumab	Antagonist	99.90%
Vedolizumab is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.

HY-17369B

Tirofiban	Antagonist	99.88%
Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.

HY-108831

Natalizumab	Antagonist	≥99.10%
Natalizumab is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.

HY-124290

Carotegrast methyl	Antagonist	99.24%
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.

HY-15770

TR-14035	Antagonist	98.06%
TR-14035 is a orally active dual α₄β₇/α₄β₁ integrin antagonist, with IC₅₀ s of 7 nM and 87 nM for α₄β₇ and α₄β₁, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.

HY-17369

Tirofiban hydrochloride monohydrate	Antagonist	99.99%
Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area.

HY-19767A

GSK 3008348 hydrochloride	Antagonist	99.86%
GSK 3008348 hydrochloride is a small molecule integrin αvβ6 antagonist, extracted from patent WO/2014154725A1, example 1. The affinity (pIC50) for the human - a 6 protein in the Fluorescence Polarisation Assay for GSK 3008348 (hydrochloride) is 8.1, whereas its affinity in the cell Adhesion Assays was for: ανβ6 (pIC50 = 8.4); ανβ3 (pIC50 = 6); ανβ5 (pIC50 = 6.9); ανβ8 (pIC50 = 7.7).

HY-19307

SB-273005	Antagonist	99.94%
SB-273005 is an orally active non-peptide αvβ3 integrin antagonist with K_i values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .

HY-14951

Firategrast	Antagonist	99.75%
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.

HY-P9911A

Vedolizumab (anti-α4β7-integrin)	Antagonist	99.90%
Vedolizumab (anti-α4β7-integrin) is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.

HY-108831A

Natalizumab (Solution)	Antagonist	98.72%
Natalizumab (Solution) is a recombinant, humanized IgG4 monoclonal antibody, binds to α4β1-integrin and blocks its interaction with vascular cell adhesion molecule-1 (VCAM-1). Natalizumab can be used for the treatment of relapsing remitting multiple sclerosis and Crohn's disease. Natalizumab is also the first targeted therapy which blocks an essential mechanism for lymphocyte entry to the CNS and thus prevents acute demyelinating relapses.

HY-W008859

Tetrac	Antagonist	99.21%
Tetrac (Tetraiodothyroacetic acid), a derivative of L-thyroxine (T4), is a thyrointegrin receptor antagonist. Tetrac blocks the actions of T4 and 3,5,3'-triiodo-L-thyronine (T3) at the cell surface receptor for thyroid hormone on integrin αvβ3. Tetra has anti-angiogenic and anti-tumor activities.

HY-120628

BMS-587101	Antagonist	99.39%
BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research.

HY-W588250

Surfactin C1	Antagonist	99.36%
Surfactin C1 is an amphiphilic biosurfactants. Surfactin C1 inhibits leukemic cell (HL-60) adhesion to human umbilical vein endothelial cells (HUVEC). Surfactin C1 inhibits adhesion melecules expression, such as ICAM-1 and VCAM-1.

HY-P1189A

Echistatin TFA	Antagonist	98.05%
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of α_IIbβ₃, α_vβ₃ and α₅β₁.

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