(E)-Elafibranor

Research use only, not for human use.

R112 is an ATP-competitive inhibitor of Syk kinase.

R112 is a Syk inhibitor. R112 inhibited degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC(50)] = 353 nmol/L) or basophils (histamine release, EC(50) = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC(50) = 490 nmol/L). R112 also blocked leukotriene C4 production and all proinflammatory cytokines tested. Subsequent molecular characterization indicated that R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor (inhibitory constant [K(i)] = 96 nmol/L).

R112; R112; R 112

Others

Other Targets

Syk

Inflammation/Immunology

——

575474-82-7

312.3

C16H13FN4O2

98%

DMSO : ≥ 41 mg/mL; 131.28 mM

c1cc(cc(c1)O)Nc1nc(ncc1F)Nc1cc(ccc1)O

3,3'-((5-fluoropyrimidine-2,4-diyl)bis(azanediyl))diphenol

(-20℃)

With Ice Pack

≥ 2 years