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  3. Lifitegrast

Lifitegrast (Synonyms: SAR 1118; SHP-606)

Cat. No.: HY-19344 Purity: 99.58%
Handling Instructions

Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.

For research use only. We do not sell to patients.

Lifitegrast Chemical Structure

Lifitegrast Chemical Structure

CAS No. : 1025967-78-5

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10 mM * 1  mL in DMSO USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 66 In-stock
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50 mg USD 200 In-stock
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100 mg USD 330 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.

IC50 & Target

IC50: 2.98 nM (LFA-1)[1]

In Vitro

Lifitegrast (SAR 1118) 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 (SAR 1118) strongly inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM[1].

In Vivo

Lifitegrast (SAR 1118), 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 (SAR 1118) to the corneal surface of healthy adults is safe and well tolerated[2]. Lifitegrast (SAR 1118) ophthalmic drops administered thrice daily deliver therapeutic levels of Lifitegrast (SAR 1118) in the retina and can alleviate the retinal complications associated with diabetes[3].

Clinical Trial
Molecular Weight

615.48

Formula

C₂₉H₂₄Cl₂N₂O₇S

CAS No.

1025967-78-5

SMILES

O=C(O)[[email protected]](CC1=CC=CC(S(=O)(C)=O)=C1)NC(C2=C(Cl)C3=C(CN(C(C4=CC=C5C=COC5=C4)=O)CC3)C=C2Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 29 mg/mL (47.12 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6247 mL 8.1237 mL 16.2475 mL
5 mM 0.3249 mL 1.6247 mL 3.2495 mL
10 mM 0.1625 mL 0.8124 mL 1.6247 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2][3]

Rats: The ocular pharmacokinetics of Lifitegrast (SAR 1118) are studied in rats after a single topical dose of 14C-SAR 1118 (1 mg/eye; 40 μCi; 15.5 μL). Lifitegrast (SAR 1118) concentration time profiles in plasma and ocular tissues are quantified by liquid scintillation counting (LSC). The pharmacologic activity of SAR 1118 eye drops administered thrice daily for 2 months at 1% (0.3 mg/eye/d) and 5% (1.5 mg/eye/d) is assessed in an STZ-induced diabetic rat model by determining retinal leukostasis and blood–retinal barrier breakdown[3].

Mice: The role of LFA-1 (CD11a/CD18) is examined either in CD18-/- mice, by intraperitoneal injection of anti-CD11a, or by topical application of lifitegrast. Corneal inflammation is induced by epithelial abrasion and exposure to either tobramycin-killed Pseudomonas aeruginosa or Staphylococcus aureus in the presence of a 2-mm-diameter punch from a silicone hydrogel contact lens. After 24 h, corneal thickness and haze are examined by confocal microscopy, and neutrophil recruitment to the corneal stroma is detected by immunohistochemistry[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

LifitegrastSAR 1118SHP-606SAR1118SAR-1118SHP606SHP 606IntegrinInhibitorinhibitorinhibit

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