Peldesine
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- CAS号:
- 133432-71-0
- 英文名:
- 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
- 中文名:
- Peldesine
- 中文别名:
- 培得星;化合物 T12399;化合物PELDESINE
- CBNumber:
- CB61116465
- 分子式:
- C12H11N5O
- 分子量:
- 241.25
- MOL File:
- 133432-71-0.mol
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Peldesine性质、用途与生产工艺
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。
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
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
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Cell Line:
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Jurkat cells
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Concentration:
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0 µM, 10 µM, 20 µM, 30 µM, 40 µM, 50 µM
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Incubation Time:
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72 hours
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Result:
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In the presence of 10 µM dCuo, had a complete inhibitory effect for T-cell lines.
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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).
Peldesine
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-106934 | Peldesine | | 1 mg | 1590元 |
| 2024/04/30 | HY-106934 | Peldesine
Peldesine | 133432-71-0 | 5mg | 3500元 |
133432-71-0, Peldesine 相关搜索:
- 化合物PELDESINE
- 培得星
- 化合物 T12399
- 133432-71-0
- 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
- 4H-Pyrrolo[3,2-d]pyrimidin-4-one, 2-amino-3,5-dihydro-7-(3-pyridinylmethyl)-
- BCX 34
- Peldesine