Potent negative allosteric modulator of LFA-1 (lymphocyte function-associated antigen-1) (Kd = 26 nM). Binds to the I-domain of LFA-1. Reversibly inhibits LFA-1 mediated binding of SKW3 leukemia cells to ICAM-1. Inhibits superantigen (SEB)-induced IL-2 production from lymphocytes in vitro and attenuates the SEB-induced increase in IL-2 plasma levels in a mouse model in vivo. Orally available.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 442.13. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.26 mL||11.31 mL||22.62 mL|
|5 mM||0.45 mL||2.26 mL||4.52 mL|
|10 mM||0.23 mL||1.13 mL||2.26 mL|
|50 mM||0.05 mL||0.23 mL||0.45 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Kelly et al (1999) Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion. J.Immunol. 163 5173 PMID: 10553036
Wu et al (2004) Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives. J.Med.Chem. 47 5356 PMID: 5481974
Last-Barney et al (2001) Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction. J.Am.Chem.Soc. 123 5643 PMID: 11403595
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