133432-71-0
133432-71-0 結(jié)構(gòu)式
基本信息
化合物 T12399
化合物PELDESINE
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
常見問題列表
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
| 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. |
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).