BIRT 377

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Cat.No. 4776 - BIRT 377 | C18H15BrCl2N2O2 | CAS No. 213211-10-0
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 (1)
Literature (3)

Biological Activity

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.

Compound Libraries

BIRT 377 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 44.21 100
ethanol 22.11 50

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 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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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

1 Citation 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

Do you know of a great paper that uses BIRT 377 from Tocris? Please let us know.

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Literature in this Area

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A collection of over 190 products for immunology research, the guide includes research tools for the study of:

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  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
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Enabling Research By Provision of Chemical Tools

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.