Peldesine dihydrochloride(Synonyms: BCX 34 dihydrochloride)

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Peldesine dihydrochloride (Synonyms: BCX 34 dihydrochloride) 纯度: 99.80%

Peldesine (BCX 34) dihydrochloride 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 dihydrochloride 还是一种 T 细胞 (T-cell) 增殖抑制剂，IC50 为 800 nM。Peldesine dihydrochloride 可用于皮肤 T 细胞淋巴瘤，牛皮癣和 HIV 感染的研究。

Peldesine dihydrochloride(Synonyms: BCX 34 dihydrochloride)

Peldesine dihydrochloride Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4620 In-stock
5 mg ￥4200 In-stock
10 mg ￥7000 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research[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 IC50 of 0.57 μM but not rat or mouse T-cell proliferation up to 30 μM[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Jurkat cells
Concentration: 0-50 µM
Incubation Time: 72 hours
Result: In the presence of 10 µM dCuo, had a complete inhibitory effect for T-cell lines.

Clinical Trial

分子量

314.17

Formula

C12H13Cl2N5O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 200 mg/mL (636.60 mM; Need ultrasonic)

H2O : 33.33 mg/mL (106.09 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1830 mL 15.9150 mL 31.8299 mL
5 mM 0.6366 mL 3.1830 mL 6.3660 mL
10 mM 0.3183 mL 1.5915 mL 3.1830 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Wada Y, et al. BCX-34: a novel T-cell selective immunosuppressant: purine nucleoside phosphorylase (PNP) inhibitor. Artif Organs. 1996 Aug;20(8):849-52.

    [2]. Duvic M, et al. A phase III, randomized, double-blind, placebo-controlled study of peldesine (BCX-34) cream as topical therapy for cutaneous T-cell lymphoma. J Am Acad Dermatol. 2001 Jun;44(6):940-7.

    [3]. Bantia S, et al. In vivo and in vitro pharmacologic activity of the purine nucleoside phosphorylase inhibitor BCX-34: the role of GTP and dGTP. Immunopharmacology. 1996 Oct;35(1):53-63.

    [4]. New AIDS study suppresses T cells to stop viral growth. AIDS Alert. 1997 Jul;12(7):77-8.

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