Peldesine,133432-71-0

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Peldesine

CAS No. : 133432-71-0

MCE 国际站：Peldesine

产品活性：Peldesine (BCX 34) 是一种有效的，竞争性，可逆和口服活性的嘌呤核苷磷酸化酶 (PNP) 抑制剂，对人，大鼠和小鼠红细胞 (RBC) PNP 的 IC₅₀ 分别为 36 nM，5 nM 和 32 nM。Peldesine 还是一种 T 细胞 (T-cell) 增殖抑制剂，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。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection

作用靶点：Nucleoside Antimetabolite/Analog  |  HIV

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

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).

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