BMS-566419

BMS-566419 is an orally active IMPDH inhibitor with an IC₅₀ of 91 nM against human IMPDH I and 68 nM against human IMPDH II. BMS-566419 exerts anti-heart transplant rejection and anti-renal fibrosis effects, and inhibits the expression of MCP-1, TGF-β1 as well as antibody production. BMS-566419 can be used in research on renal fibrosis and organ transplantation^[1][2]. In Vitro:BMS-566419 (48 h) inhibits Concanavalin A (HY-P2149)-stimulated splenic T cell proliferation in Lewis rats, with an IC₅₀ of 320 nM^[1].
BMS-566419 (48 h) inhibits the proliferation of LPS (HY-D1056)-stimulated B cells from the spleen of Lewis rats, with an IC₅₀ of 230 nM^[1].
BMS-566419 (72 h) inhibits allogeneic antigen-specific proliferation of T cells from Lewis rats in mixed lymphocyte reactions, with an IC₅₀ of 95 nM^[1].
BMS-566419 (10-1000 nM; 72 h) inhibits IgM production in LPS-stimulated splenic B cells from Lewis rats in vitro, with an IC₅₀ of 170 nM^[1]. In Vivo:BMS-566419 (10-60 mg/kg; p.o.; 14 days) significantly prolongs the median survival time of rat heart transplants at doses of 30 and 60 mg/kg, to 10 days and 18 days respectively, and exhibits better efficacy when co-administered with Tacrolimus (HY-13756)^[1].
BMS-566419 (30-60 mg/kg; p.o.; 4 days) significantly inhibits T-cell-independent anti-DNP IgM antibody production in rats, with a maximum inhibition rate of over 95%^[1].
BMS-566419 (60 mg/kg; p.o.; 7 days) significantly inhibits the production of alloantigen-specific IgM and IgG1/2a antibodies in rats, with inhibition rates of 70% and 96%, respectively^[1].
BMS-566419 (30-60 mg/kg; p.o.; 14 days) exerts a dose-dependent inhibitory effect on renal fibrosis induced by UUO in rats^[2].