Pentamidine isethionate (Synonyms:喷他脒羟乙磺酸盐; MP-601205 isethionate)
目录号 : KM12342 CAS No. : 140-64-7 纯度 : 98%

Pentamidine isethionate (MP-601205 isethionate) 是一种抗微生物剂,会干扰 DNA 的生物合成。Pentamidine isethionate 抑制寄生虫 Leishmania infantum,IC50 为 2.5 μM。Pentamidine isethionate 是一种有效的选择性蛋白酪氨酸磷酸酶 (PTPases) 和再生肝磷酸酶 (PRL) 抑制剂。Pentamidine isethionate 可用于冈比亚锥虫病,抗锑利什曼病和卡氏肺孢子虫肺炎的研究。抗肿瘤活性,抗菌活性。

规格 价格 是否有货 数量
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

体外研究

Pentamidine (0-10 µg/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth of cancer cells in a concentration-dependent manner.
The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite Leishmania infantum is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h of incubation than that of Cisplatin. Pentamidine isethionate induces a higher amount of programmed cell death (PCD) than Cisplatin, which is associated with inhibition of DNA synthesis and cell-cycle arrest in the G2/M phase. Binding of Pentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix, consistent with a B-->A transition. The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase in the beta-sheet content of the protein.

Cell Viability Assay

Cell Line: WM9, DU145, C4-2, Hey, WM480, and A549 cells
Concentration: 0-10 µg/mL
Incubation Time: 6 days
Result: The growth of all six of the cell lines in culture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10 µg/mL.
体内研究

Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatment markedly inhibits the growth of WM9 human melanoma tumors in nude mice.

Animal Model: Athymic nude mice (6 weeks old) injected with WM9 cells
Dosage: 0.25 mg/mouse
Administration: Intramuscular injection; every 2 days; for 4 weeks
Result: Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.
分子式
C23H36N4O10S2
分子量
592.68
CAS号
140-64-7
中文名称
喷他脒羟乙磺酸盐;依西酸喷他脒;戊双氧苯脒;
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

H2O : 100 mg/mL (168.73 mM; Need ultrasonic)

DMSO : 100 mg/mL (168.73 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6873 mL 8.4363 mL 16.8725 mL
5 mM 0.3375 mL 1.6873 mL 3.3745 mL
10 mM 0.1687 mL 0.8436 mL 1.6873 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 (protect from light)。-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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.51 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.51 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.51 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.51 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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: ≥ 2.08 mg/mL (3.51 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.51 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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科研文献
The molarity calculator equation
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