BIRT 377

Cat. No. 4776 4 Citations Submit a Review Datasheet / COA / SDS

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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)

Datasheet

Citations (4)

Reviews

Literature (2)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for BIRT 377

BIRT 377 is a potent negative allosteric modulator of LFA-1 (lymphocyte function-associated antigen-1) (K_d = 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
InChI Key	FJNJHZQMQRVZEE-GOSISDBHSA-N
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
Solubility
	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.

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

Safety Datasheet

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:

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

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

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

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

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

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Angiogenesis in Cancer Poster

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

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.