| 名称 | Peldesine |
| 描述 | Peldesine (BCX 34) 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. |
| 体外活性 | 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]. |
| 体内活性 | Peldesine demonstrates oral efficacy by elevating plasma inosine levels in rats (2-fold at 30 mg/kg), significantly reducing ex vivo red blood cell (RBC) purine nucleoside phosphorylase (PNP) activity in rats (98% at 3 hours, 100 mg/kg), and moderately suppressing ex vivo skin PNP activity in mice (39% at 3 hours, 100 mg/kg). Additionally, Peldesine exhibits an oral bioavailability of 76% in rats[2]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 195 mg/mL (808.29 mM), Sonication is recommended.
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| 关键字 | Inhibitor | inhibit | PNP | inosine | dGuo | Peldesine | HIV | Nucleoside | psoriasis | Nucleoside Antimetabolite/Analog | phosphorylase | Human immunodeficiency virus | lymphoma | IL-2 | T-cell | BCX-34 | immunosuppressive | BCX34 |
| 相关产品 | Stavudine | 5-Fluorouracil | Inosine pranobex | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 4500-5500) | Lamivudine | Chloroquine phosphate | Tenofovir Disoproxil Fumarate | Decanedioic acid | Tenofovir |
| 相关库 | 经典已知活性库 | ReFRAME 相关化合物库 | 药物功能重定位化合物库 | 抗病毒库 | 抑制剂库 | 口服活性化合物库 | 临床期小分子药物库 | 已知活性化合物库 | 人代谢物化合物库 |
United States
