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)
Datasheet
Citations (1)
Reviews
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

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Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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.

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

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


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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


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