BIRT 377
Chemical Name: (5R)-5-[(4-Bromophenyl)methyl]-3-(3,5-dichlorophenyl)-1,5-dimethyl-2,4-imidazolidinedione
Purity: ≥98%
Biological Activity
BIRT 377 is a potent negative allosteric modulator of LFA-1 (lymphocyte function-associated antigen-1) (Kd = 26 nM). BIRT 377 binds to the I-domain of LFA-1. BIRT 377 reversibly inhibits LFA-1 mediated binding of SKW3 leukemia cells to ICAM-1. BIRT 377 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.Technical Data
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
Wu et al.
J.Med.Chem., 2004;47:5356 -
Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion.
Kelly et al.
J.Immunol., 1999;163:5173 -
Binding site elucidation of hydantoin-based antagonists of LFA-1 using multidisciplinary technologies: evidence for the allosteric inhibition of a protein--protein interaction.
Last-Barney et al.
J.Am.Chem.Soc., 2001;123:5643
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Citations for BIRT 377
The citations listed below are publications that use Tocris products. Selected citations for BIRT 377 include:
2 Citations: Showing 1 - 2
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Anti-aLβ2 antibodies reveal novel endocytotic cross-modulatory functionality.
Authors: Mancuso Et al.
Br.J.Pharmacol. 2020;177:2696
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LFA-1 antagonist (BIRT377) similarly reverses peripheral neuropathic pain in male and female mice with underlying sex divergent peripheral immune proinflammatory phenotypes.
Authors: Noor Et al.
Neuroimmunol Neuroinflammation 2019;6:11
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