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Lifitegrast is an antagonist of integrin lymphocyte function associated antigen-1 (LFA-1). The IC50 of Jurkat T cells to icAM-1 was 2.98nM. Lifitegrast blocks the interaction between LFA-1 and ICAM-1, thereby reducing T cell activity and cytokine secretion.
In vitro: Lifitegrast is a novel small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), thus lessening overall inflammatory responses. Lifitegrast strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
In vivo: Lifitegrast, has potent anti-inflammatory activity on corneal inflammation induced by antibiotic-killed P. aeruginosa and S. aureus in the presence of a silicone hydrogel lens with the optimal application being a 1% solution applied either 2 or 3 times prior. Topical application of lifitegrast to the corneal surface of healthy adults is safe and well tolerated. SAR 1118 ophthalmic drops administered thrice daily deliver therapeutic levels of SAR 1118 in the retina and can alleviate the retinal complications associated with diabetes.
| Cell Experiment | |
|---|---|
| Cell lines | T-cell |
| Preparation method | Lifitegrast potently inhibits human T-cell binding to human ICAM-1, T-cell activation and cytokine release, and formation of the immunologic synapse. |
| Concentrations | 3 nM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | dogs diagnosed with keratoconjunctivitis sicca |
| Formulation | |
| Dosages | |
| Administration | i.v. |
| Molecular Weight | 615.48 |
| Formula | C29H24Cl2N2O7S |
| CAS Number | 1025967-78-5 |
| Solubility (25°C) | 29 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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αvβ1 integrin-IN-1 is a potent and selective αvβ1 integrin inhibitor with an IC50 of 0.63 nM. αvβ1 integrin-IN-1 has antifibrotic effects. |
| MORF-627
MORF-627 is a selective, orally active inhibitor for integrin αvβ6 with an IC50 of 9.2 nM (measuring by human serum ligand binding assay). MORF-627 inhibits αvβ6-mediated TGF-β1 activation with an IC50 of 2.63 nM, inhibits SMAD2/3 phosphorylation with an IC50 of 8.3 nM. |
| Volociximab
Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs). |
| GSK 3008348 hydrochloride
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| HSDVHK-NH2
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM). |
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