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。
生物活性 | Peldesine (BCX 34) is a potent, competitive, reversible and orally activepurine nucleoside phosphorylase (PNP)inhibitor withIC50s of 36 nM, 5 nM, and 32 nM forhuman, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also aT-cellproliferation inhibitor with anIC50of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis andHIVinfectionresearch[1][2][3][4]. |
IC50& Target | IC50: 36 nM (Human RBC PNP), 5 nM (Rat RBC PNP), 32 nM (Mouse RBC PNP), and 800 nM (Human T-cell proliferation)[3] Ki: 23 nM (Human RBC PNP)[3] HIV[4] |
体外研究 (In Vitro) | 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[1]. 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[1]. Peldesine also, in the presence but not in the absence of deoxyguanosine, inhibits human leukemia CCRF-CEM T-cell proliferation with an IC50of 0.57 μM but not rat or mouse T-cell proliferation up to 30 μM[3].
Cell Proliferation Assay[1] 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 (In Vivo) | 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)[3].
|
Clinical Trial | |
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : 200 mg/mL(829.02 mM;Need ultrasonic) 配制储备液 1 mM | 4.1451 mL | 20.7254 mL | 41.4508 mL | 5 mM | 0.8290 mL | 4.1451 mL | 8.2902 mL | 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 5 mg/mL (20.73 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (20.73 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 5 mg/mL (20.73 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (20.73 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (20.73 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (20.73 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|