AS041164
5-(Benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive, and isoform-selctive PI 3-K inhibitor (IC50 = 0.07, 0.24, 1.45, and 1.70 µM for the g, a, b, and d isoform, respectively) with little or no activity against a panel of 38 other commonly studied kinases (<20% inhibition at 1.0 µM). Exhibits similar pharmacokinetics as LY 294002 (Cat. Nos. 440202 & 440204) via oral administration, but is 3-times as potent (ED50 = 27.35 mg/kg, p.o.) in blocking rhRNATES-induced neutrophil peritoneal recruitment in mice in vivo. Also reported to exhibit significant in vivo prophylactic efficacy against carrageenan-induced tissue swelling in a rat paw edema model (100 mg/kg, p.o.). Purity: ≥98% by HPLC. Ref.: Ferrandi, C., et al. 2007. J. Pharmacol. Exp. Ther. 322, 923.
R: 43; S: 36/37-45 |
