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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Integrin Products |
|---|
| HSDVHK-NH2
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM). |
| LDV
LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC. |
| Cyclo(RADfK)
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. |
| Obtustatin
Obtustatin is a non-RGD disintegrin of 41 residues. |
| Integrin Binding Peptide
Integrin Binding Peptide is derived by fibronectin. |
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