EOS200271

EOS200271 is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1, IC50 = 0.15 µM for the human enzyme). It is selective for IDO-1 over IDO-2 up to a concentration of 200 µM for the human recombinant enzymes. EOS200271 inhibits IDO-1-mediated production of kynurenine induced by IFN-gamma in HeLa cells (IC50 = 1.8 µM) and by LPS and IFN-gamma in THP-1 cells and human-derived whole blood ex vivo (IC50s = 1.7 and 4.7 µM, respectively).Formal Name: 3-(5-fluoro-1H-indol-3-yl)-2,5-pyrrolidinedione. CAS Number: 198474-05-4. Synonyms: PF-06840003. Molecular Formula: C12H9FN2O2. Formula Weight: 232.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 221, 287 nm. SMILES: FC1=CC=C2C(C(C3CC(NC3=O)=O)=CN2)=C1. InChi Code: InChI=1S/C12H9FN2O2/c13-6-1-2-10-7(3-6)9(5-14-10)8-4-11(16)15-12(8)17/h1-3,5,8,14H,4H2,(H,15,16,17). InChi Key: MXKLDYKORJEOPR-UHFFFAOYSA-N.