Integrin

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.

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

RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist.

BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1).

Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist.

Valategrast hydrochloride (R-411) is a potent integrin α4β1 (VLA-4) and α4β7 dual antagonist.

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

αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) .

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

Abciximab, a chimeric (murine/human) monoclonal antibody fragment (c7E3 Fab), is a glycoprotein IIb/IIIa antagonist.

Bexotegrast is a potent inhibitor of αΝβ6 integrin. Bexotegrast can be used for researching fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP) (extracted from patent WO2020210404A1, compound 5).

Abituzumab (DI17E6) is a humanized monoclonal antibody (IgG2 type) against integrin αV. Abituzumab can effectively reduce the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, especially for prostate cancer.

Bersanlimab (BI-505) is a fully human monoclonal antibody that targets intercellular adhesion molecule-1 (ICAM-1 or CD54). Bersanlimab has anti-cancer effects.

Certepetide (CEND-1) is a novel tumor-targeting internalized arginine-glycine bifunctional cyclic peptide (a.k.a. iRGD), which is being developed for the treatment of solid tumors.

Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) TFA is a cyclic RGD peptide with high affinity for αvβ3 integrin, which can disrupt cell adhesion. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA inhibits the expression of pluripotency genes in embryonic stem cells (ESC), and suppresses the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA can be used for tumor-related research.

Efalizumab is a targeted T-cell modulator, which is a humanized monoclonal antibody against the LFA-1 alpha subunit CD11a. Efalizumab can inhibit T-cell activation, skin T-cell trafficking and T-cell adhesion to keratinocytes, and can be used in research on plaque psoriasis.

EMD527040 is a highly efficient and selective αvβ6 antagonist with anti-fibrotic activity. It can be used for research on liver cancer and liver fibrosis.

Enlimomab (BI-RR 0001) is a mouse IgG2a monoclonal antibody targeting human ICAM-1, which can inhibit leukocyte adhesion to vascular endothelium, thereby reducing leukocyte extravasation and inflammatory tissue damage. Enlimomab has anti-inflammatory effects and can be used in stroke research.

Orbofiban acetate is an orally active platelet membrane glycoprotein IIb/IIIa antagonist that inhibits platelet aggregation.

(R/S)-Alicaforsen is the racemic form of Alicaforsen, which consists of both R and S configurations. Alicaforsen is a 20-base length antisense oligonucleotide that inhibits the production of ICAM-1, an important adhesion molecule involved in the migration and transport process of white blood cells to inflammatory sites.