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133432-71-0

中文名称 Peldesine
英文名称 Peldesine
CAS 133432-71-0
分子式 C12H11N5O
分子量 241.25
MOL 文件 133432-71-0.mol
更新日期 2023/03/20 15:41:21
133432-71-0 结构式 133432-71-0 结构式

基本信息

中文别名
培得星
化合物 T12399
化合物PELDESINE
英文别名
BCX 34
Peldesine
4H-Pyrrolo[3,2-d]pyrimidin-4-one, 2-amino-3,5-dihydro-7-(3-pyridinylmethyl)-
Inhibitor,inhibit,PNP,inosine,dGuo,HIV,Nucleoside,psoriasis,Nucleoside Antimetabolite/Analog,phosphorylase,Human immunodeficiency virus,lymphoma,IL-2,T-cell,BCX-34,Peldesine,BCX34,immunosuppressive

物理化学性质

储存条件-20°C储存
形态Solid
颜色Light yellow to yellow
Peldesine价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/02/08HY-106934Peldesine133432-71-01 mg1590元
2025/02/08HY-106934Peldesine
Peldesine
133432-71-05mg3500元
2025/02/08HY-106934Peldesine
Peldesine
133432-71-010mM * 1mLin DMSO3850元

常见问题列表

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).

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