BIRT 377

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Description: Potent negative allosteric modulator of LFA-1
Chemical Name: (5R)-5-[(4-Bromophenyl)methyl]-3-(3,5-dichlorophenyl)-1,5-dimethyl-2,4-imidazolidinedione
Purity: ≥98% (HPLC)
Citations (4)
Literature (2)

Biological Activity for BIRT 377

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 for BIRT 377

M. Wt 442.13
Formula C18H15BrCl2N2O2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 213211-10-0
PubChem ID 9803375
Smiles CN([C@@](CC3=CC=C(Br)C=C3)(C)C(N1C2=CC(Cl)=CC(Cl)=C2)=O)C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BIRT 377

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 44.21 100
ethanol 8.84 20

Preparing Stock Solutions for BIRT 377

The following data is based on the product molecular weight 442.13. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for BIRT 377

Certificate of Analysis / Product Datasheet
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References for BIRT 377

References are publications that support the biological activity of the product.

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: 15481974

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

If you know of a relevant reference for BIRT 377, please let us know.

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Keywords: BIRT 377, BIRT 377 supplier, BIRT377, potent, negative, allosteric, modulators, LFA-1, lymphocyte, function-associated, antigen-1, cell, adhesion, orally, available, integrins, NAM, Integrins, Cell, Adhesion, Molecules, 4776, Tocris Bioscience

4 Citations for BIRT 377

Citations are publications that use Tocris products. Selected citations for BIRT 377 include:

Noor et al (2019) LFA-1 antagonist (BIRT377) similarly reverses peripheral neuropathic pain in male and female mice with underlying sex divergent peripheral immune proinflammatory phenotypes. Neuroimmunol Neuroinflammation 6 11 PMID: 31763376

Yu et al (2022) C3aR Signaling Inhibits NK-cell Infiltration into the Tumor Microenvironment in Mouse Models. Cancer Immunol Res 10 245-258 PMID: 34819308

Erin D et al (2020) The LFA-1 antagonist BIRT377 reverses neuropathic pain in prenatal alcohol-exposed female rats via actions on peripheral and central neuroimmune function in discrete pain-relevant tissue regions. Brain Behav Immun 87 339-358 PMID: 31918004

Mancuso et al (2020) Anti-aLβ2 antibodies reveal novel endocytotic cross-modulatory functionality. Br.J.Pharmacol. 177 2696 PMID: 31985813

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

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This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Enabling Research By Provision of Chemical Tools Poster

Enabling Research By Provision of Chemical Tools Poster

The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.