Effect of the inosine 5′-monophosphate dehydrogenase inhibitor BMS-566419 on rat cardiac allograft rejection

Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3

“…An in vivo rat heterotopic cardiac transplant model was investigated using ACI rats as cardiac donors and Lewis rats as cardiac recipients, and median survival times (MST) of grafts were analyzed. 30 Lead compound 2 inhibited JAK3 (IC 50 = 5.1 nM) and T cell proliferation (IC 50 = 86 nM).…”

“…31 was also evaluated for in vivo efficacy to prevent allograft rejection in a rat heterotopic cardiac transplantation model 30 (Table 6). In this model, untreated allografts were ultimately rejected with a graft survival period of five days after transplantation.…”

“…In addition, the efficacy of 31 was investigated in an in vivo rat heterotopic cardiac transplant model. 30 …”

Release mechanisms of tacrolimus-loaded PLGA and PLA microspheres and immunosuppressive effects of the microspheres in a rat heart transplantation model

“…3 are summarized in Table 3. The beat of the transplanted heart stops within 5-6 days without treatment in this model (Nakanishi et al, 2010). The graft-survival rates were 0, 57, and 100% at a dose of 0.75, 3.0, and 7.5 mg/kg, respectively.…”

Effect of the inosine 5′-monophosphate dehydrogenase inhibitor BMS-566419 on renal fibrosis in unilateral ureteral obstruction in rats

“…The oral efficacy of BMS-566419 has been confirmed in an experimental autoimmune disease model [26]. Recently, we reported that BMS-566419 was also effective for the prevention of acute rejection in a rat cardiac transplant model, with equivalent efficacy to MMF [27]. However, the question of whether these newly synthesized IMPDH inhibitors have an antifibrotic effect, similar to that of MMF, remains unanswered.…”