Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC 50 s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP , respectively. Peldesine is also a T-cell proliferation inhibitor with an IC 50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research
In Vitro
Peldesine (BCX 34; 0-50 µM; 72 hours; Jurkat cells) could inhibit the T-cell proliferation completely at a concentration of less than 10 μM, in the presence of dGuo (10 μM). In contrast, the B-cell proliferation is not affected by Peldesine. Peldesine (BCX 34) suppresses T-cell immune reaction in an IL-2-independent manner, and this means that Peldesine might affect a late phase rather than an early stage in T-cell activation. Peldesine also, in the presence but not in the absence of deoxyguanosine, inhibits human leukemia CCRF-CEM T-cell proliferation with an IC 50 of 0.57 μM but not rat or mouse T-cell proliferation up to 30 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Jurkat cells Concentration: 0 µM, 10 µM, 20 µM, 30 µM, 40 µM, 50 µM Incubation Time: 72 hours Result: In the presence of 10 µM dCuo, had a complete inhibitory effect for T-cell lines.
In Vivo
Oral bioavailability of Peldesine in rats is 76%. Peldesine is orally active in elevating plasma inosine in rats (2-fold at 30 mg/kg), in suppressing ex vivo RBC PNP activity in rats (98% at 3 h. 100 mg/kg), and in suppressing ex vivo skin PNP in mice (39% at 3 h, 100 mg/kg). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 36 nM (Human RBC PNP), 5 nM (Rat RBC PNP), 32 nM (Mouse RBC PNP), and 800 nM (Human T-cell proliferation), Ki: 23 nM (Human RBC PNP),HIV
