Peldesine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Peldesine 是一种有效的、竞争性的、可逆的、口服活性的嘌呤核苷磷酸化酶抑制剂。

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