羟乙基磺酸喷他脒（0-10 μg/mL；6 天；WM9、DU145、C4-2、Hey、WM480 和 A549 细胞）治疗可以浓度调节的方式抑制糖尿病的生长 [1]。已确定羟乙基磺酸喷他脒对动物寄生虫利什曼原虫前鞭毛体的危害程度。乙磺酸喷他脒在 72 小时无菌期后表现出比顺铂高 60 倍的杀利什曼活性。 G2/M 期 DNA 合成和细胞周期信号传导的抑制是喷他脒羟乙基磺酸盐比顺铂引起更多程序性细胞死亡 (PCD) 的原因。小牛胸腺 DNA (CT-DNA) 响应喷他脒羟乙磺酸盐结合而发生构象变化，这与 B→A 转变一致。 Pentamidine isethionate 相当于泛素，可使蛋白质的 β-折叠含量增加 6% [2]。

羟乙基磺酸喷他脒（0.25 mg/小鼠；肌内注射；每 2 天一次；持续 4 周；无胸腺裸鼠）治疗显着抑制细胞内 WM9 人黑色素瘤生长 [1]。

细胞活力测定[1]
细胞类型： WM9、DU145、C4-2、Hey、WM480 和 A549 细胞
测试浓度： 0-10 µg/mL
孵育时间： 6 天
实验结果： 培养物中所有六种细胞系的生长 以浓度依赖性方式受到抑制，且完全抑制10 µg/mL 下的细胞系生长。

Animal/Disease Models: Athymic nude mice (6 weeks old) were injected with WM9 cells [1].
Doses: 0.25 mg/mouse.
Route of Administration: intramuscularinjection; once every 2 days; for 4 consecutive weeks.
Experimental Results: Dramatically inhibited the growth of WM9 human melanoma in nude mice. Growth in mice.

[1]. Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64.

[2]. Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400.

[3]. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34.

[4]. Pentamidine: a drug to consider re-purposing in the targeted treatment of multi-drug resistant bacterial infections? J Lab Precis Med 2017;2:49.

Pentamidine isethionate appears as odorless white or almost white crystals or powder. Odor also reported as a slight butyric odor. Very bitter taste. pH (5% aqueous solution) 4.5-6.5. (NTP, 1992)
Pentamidine isethionate is an organosulfonate salt obtained by reaction of pentamidine with two equivalents of 2-hydroxyethylsulfonic acid. It has a role as a trypanocidal drug. It contains a pentamidinium(2+).
Pentamidine isethionate is an antifungal prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment and prevention of Pneumocystis pneumonia (PCP).  The FDA-approved uses for pentamidine isethionate depend on the dosage form of the drug. Specifically, pentamidine isethionate injection is approved to treat PCP, and pentamidine isethionate inhalant is approved to prevent PCP in people with HIV who are at high risk of developing PCP.
PCP can be an opportunistic infection (OI) of HIV.
Pentamidine Isethionate is a synthetic amidine derivative, Pentamidine Isethionate is an antiprotozoal and antifungal agent that appears to interact with the minor groove of AT-rich DNA regions of the pathogen genome, interfering with DNA replication and function. It is effective in the treatment of trypanosomiasis, leishmaniasis, some fungal infections, and Pneumocystis carinii pneumonia in HIV-infected patients. (NCI04)
Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects.
See also: Pentamidine (has active moiety).

C23H36N4O10S2

592.68

592.187

140-64-7

Pentamidine;100-33-4;Pentamidine dihydrochloride;50357-45-4;Pentamidine dimesylate;6823-79-6

8813

White to off-white solid powder

539.4ºC at 760mmHg

188-194 °C(lit.)

280ºC

1.06E-11mmHg at 25°C

4.377

284.16

8

12

14

39

493

0

YBVNFKZSMZGRAD-UHFFFAOYSA-N

InChI=1S/C19H24N4O2.2C2H6O4S/c20-18(21)14-4-8-16(9-5-14)24-12-2-1-3-13-25-17-10-6-15(7-11-17)19(22)23;2*3-1-2-7(4,5)6/h4-11H,1-3,12-13H2,(H3,20,21)(H3,22,23);2*3H,1-2H2,(H,4,5,6)

4-[5-(4-carbamimidoylphenoxy)pentoxy]benzenecarboximidamide;2-hydroxyethanesulfonic acid

Pentamidine diisethionate Pentamidine isethionate salt Pentamidine Isethionate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~168.73 mM)
DMSO : ~100 mg/mL (~168.73 mM)

配方 1 中的溶解度: ≥ 2.08 mg/mL (3.51 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 20.8 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.08 mg/mL (3.51 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.08 mg/mL (3.51 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 20.8 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。