Peldesine

Research use only, not for human use.

Peldesine is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase.

Peldesine is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.(In Vitro):The IC50s are 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell purine nucleoside phosphorylase, respectively. In Jurkat cells, Peldesine (BCX 34; 0-50 μM; 72 hours) inhibits 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.(In Vivo):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). Oral bioavailability of Peldesine in rats is 76%.

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 IC50 of 0.57 μM but not rat or mouse T-cell proliferation up to 30 μM. Cell Proliferation Assay Cell 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.

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).

BCX 34

Others

Other Targets

GSTP1| Gutathione S-transferase

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133432-71-0

241.254

C12H11N5O

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (829.02 mM)

Nc1nc2c(Cc3cccnc3)c[nH]c2c(=O)[nH]1

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(-20℃)

With Ice Pack

≥ 2 years