BIRT 377

Name: BIRT 377
Brand: Tocris Bioscience
SKU: 4776

Tocris Bioscience, part of Bio-Techne | Catalog # 4776

Citations (19)

COA / SDS

Potent negative allosteric modulator of LFA-1

Key Product Details

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)
Molecular Weight:	442.13

View Full Technical Details for BIRT 377

Technical Data
Citations

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 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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References for BIRT 377

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