BIRT 377

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

2 1 Recalculate

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

Calculators

Background References

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

• Wu Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives. J.Med.Chem. 2004 PMID: 15481974
• Last-Barney 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. 2001 PMID: 11403595
• Kelly Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion. J.Immunol. 1999 PMID: 10553036