Peldesine 是一种有效的、竞争性的、可逆的和口服活性的嘌呤核苷磷酸化酶抑制剂。 Peldesine 抑制 T 细胞增殖，IC50 为 800 nM。 Peldesine 可用于皮肤 T 细胞淋巴瘤、牛皮癣和 HIV 感染的研究。

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.

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[1].

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%[2].

133432-71-0

C12H11N5O

241.25

BCX 34

DMSO:195 mg/mL (808.29 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years