Peldesine

生物活性靶点体外研究体内研究 Peldesine 试剂级价格

Peldesine

CAS号:133432-71-0
英文名:Peldesine
中文名:Peldesine
CBNumber:CB61116465
分子式:C12H11N5O
分子量:241.25
MOL File:133432-71-0.mol

Peldesine化学性质

储存条件 :Store at -20°C
形态 :Solid
颜色 :Light yellow to yellow

Peldesine性质、用途与生产工艺

生物活性 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。
靶点

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

体外研究

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.

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.

体内研究

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).