| Name | Peldesine |
| Description | 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. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (20.73 mM), Sonication is recommended. DMSO : 195 mg/mL (808.29 mM), Sonication is recommended.
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| Keywords | T-cell | Purine nucleoside phosphorylase | psoriasis | PNP | phosphorylase | Peldesine | NucleosideAntimetabolite | Nucleoside Antimetabolite/Analog | Nucleoside Antimetabolite | Nucleoside | lymphoma | inosine | Inhibitor | inhibit | immunosuppressive | IL-2 | Human immunodeficiency virus | HIVProtease | HIV Protease | HIV | dGuo | BCX-34 | BCX34 | Analog |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Adenosine | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Lamivudine | Chloroquine phosphate | Valproic Acid | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Hematonosis Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | Inhibitor Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library | Human Metabolite Library |