Free shipping on all orders over $ 500

Lifitegrast

Cat. No. M5852
Lifitegrast Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 150 In stock
50mg USD 450 In stock
100mg USD 770 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 615.48
Formula C29H24Cl2N2O7S
CAS Number 1025967-78-5
Purity >99%
Solubility 29 mg/mL in DMSO
Storage at -20°C
References

Development of lifitegrast: a novel T-cell inhibitor for the treatment of dry eye disease.
Semba CP, et al. Clin Ophthalmol. 2016 Jun 10;10:1083-94. PMID: 27354762.

Lifitegrast Ophthalmic Solution 5.0% versus Placebo for Treatment of Dry Eye Disease: Results of the Randomized Phase III OPUS-2 Study.
Tauber J, et al. Ophthalmology. 2015 Dec;122(12):2423-31. PMID: 26365210.

Related Integrin Products
Tirofiban hydrochloride monohydrate

Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist

ATN-161

ATN-161 is a novel small peptide inhibitor of integrin α5β1; a beta integrin antagonist with antitumor activity.

Cilengitide

Cilengitide (EMD 121974, NSC 707544) is a selective inhibitor of αvβ3 integrin and αvβ5 integrin with IC50 of 1 nM and 140 nM, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Lifitegrast supplier, Integrin, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.