Pentoxifylline(Synonyms: 己酮可可碱; BL-191; PTX; Oxpentifylline)

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Pentoxifylline (Synonyms: 己酮可可碱; BL-191; PTX; Oxpentifylline) 纯度: 99.35%

Pentoxifylline (BL-191) 是一种血液流变学改善剂。Pentoxifylline 是一种具有口服活性的，非选择性的磷酸二酯酶 (PDE) 抑制剂，具有免疫调节、抗炎、血液流变学改善、抗纤溶和抗增殖作用。Pentoxifylline 可用于研究周围血管疾病、脑血管疾病和其他一些涉及局部微循环缺陷的疾病。

Pentoxifylline(Synonyms: 己酮可可碱; BL-191; PTX; Oxpentifylline)

Pentoxifylline Chemical Structure

CAS No. : 6493-05-6

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10 mM * 1 mL in DMSO ￥500 In-stock
500 mg ￥400 In-stock
1 g ￥500 In-stock
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生物活性

Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].

IC50 & Target

PDE[1]
体外研究
(In Vitro)

Pentoxifylline (0.1-50 mM; 24-48 hours) inhibits cell proliferation in a dose-dependent manner[3].
Pentoxifylline (0.5 mM; 12-36 hours) increases apoptosis and decreases autophagy levels in MDA-MB-231 cells[3].
Pentoxifylline (0.5 mM; 12-36 hours) induces autophagy in MDA-MB-231 cells[3].
Pentoxifylline (0.5 mM; 24-48 hours) blocks cell cycle at the G0/G1 phase[3].
Pentoxifylline results in high LC3-II/LC3-ratio[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 Proliferation Assay[3]

Cell Line: MDA-MB-231 cells
Concentration: 0.1 mM, 1 mM, 5 mM , 10 mM, 50 mM
Incubation Time: 24 hours, 48 hours
Result: Inhibited cell proliferation in a dose-dependent manner.

Apoptosis Analysis[3]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 mM
Incubation Time: 12 hours, 24 hours, 36 hours
Result: Induced apoptosis.

Cell Autophagy Assay[3]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 mM
Incubation Time: 24 hours, 48 hours
Result: Induced approximately 20-28% of cell autophagy.

Cell Cycle Analysis[3]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 mM
Incubation Time: 24 hours, 48 hours
Result: Induced G0/G1 phase arrest.

Western Blot Analysis[3]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 mM
Incubation Time: 24 hours, 48 hours
Result: Induced high LC3-II/LC3-ratio.

体内研究
(In Vivo)

Pentoxifylline (200 mg/kg; i.p.) has a protective effect on rats with transient global ischemia and reduces cognitive impairment[4].

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.

Animal Model: Adult male Wistar rats 12-13-weeks-old (250-300 g)[4]
Dosage: 200 mg/kg
Administration: Intraperitoneal injection, at 1hr before and 3 hr after ischemia
Result: Significantly improved the spatial memory and effects were significant different from those of sham-operated and vehicle groups.

Clinical Trial

分子量

278.31

Formula

C13H18N4O3
CAS 号

6493-05-6
中文名称

己酮可可碱；已酮可可碱
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: 

H2O : 93.3 mg/mL (335.24 mM; Need ultrasonic and warming)

DMSO : ≥ 2.8 mg/mL (10.06 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5931 mL 17.9656 mL 35.9312 mL
5 mM 0.7186 mL 3.5931 mL 7.1862 mL
10 mM 0.3593 mL 1.7966 mL 3.5931 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。-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。

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： PBS

    Solubility: 110 mg/mL (395.24 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Iffat Hassan, et al. Pentoxifylline and its applications in dermatology. Indian Dermatol Online J. 2014 Oct-Dec; 5(4): 510–516.

    [2]. A Ward, et al. Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy. Drugs. 1987 Jul;34(1):50-97.

    [3]. Yessica Cristina Castellanos-Esparza, et al. Synergistic promoting effects of pentoxifylline and simvastatin on the apoptosis of triple-negative MDA-MB-231 breast cancer cells. Int J Oncol. 2018 Apr;52(4):1246-1254.

    [4]. Shabnam Movassaghi, et al. Effect of Pentoxifylline on Ischemia- induced Brain Damage and Spatial Memory Impairment in Rat. Iran J Basic Med Sci. 2012 Sep-Oct; 15(5): 1083-1090.

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