喷他脒羟乙磺酸盐作用机制 - Medchemexpress - MCE中国

1、Product Data SheetPentamidine isethionateCat. No.: HY-B0537BCAS No.: 140-64-7分式: CHNOS分量: 592.68作靶点: Parasite; Fungal; Phosphatase; Bacterial作通路: Anti-infection; Metabolic Enzyme/Protease储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 H2O : 100 m

2、g/mL (168.73 mM; Need ultrasonic)DMSO : 100 mg/mL (168.73 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.6873 mL 8.4363 mL 16.8725 mL5 mM 0.3375 mL 1.6873 mL 3.3745 mL10 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 m

3、onths; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80

4、45% salineSolubility: 2.5 mg/mL (4.22 mM); Clear solution此案可获得 2.5 mg/mL (4.22 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.22 mM); Clear solu

5、tion此案可获得 2.5 mg/mL (4.22 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合Page 1 of 2 www.MedChemE均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.22 mM); Clear solution此案可获得 2.5 mg/mL (4.22 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L

6、25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Pentamidine isethionate (MP-601205 isethionate)种抗微物剂，会扰 DNA 的物合成。Pentamidineisethionate 抑制寄 Leishmania infantum，IC50 为 2.5 M。Pentamidine isethionate 种有效的选择性蛋酪氨酸磷酸酶 (PTPases) 和再肝磷酸酶 (PRL) 抑制剂。Pentamidine isethionate 可于冈亚锥病，抗锑利什曼病和卡肺孢肺炎的研究。

7、抗肿瘤活性，抗菌活性。IC & Target IC50: 2.5 M (Leishmania infantum)2Protein tyrosine phosphatases (PTPases)1Phosphatase of regenerating liver (PRL)1体外研究 Pentamidine (0-10 g/mL; 6 days; WM9, DU145, C4-2, Hey, WM480, and A549 cells) treatment inhibits the growth ofcancer cells in a concentration-dependent manner

8、1.The cytotoxic properties of Pentamidine isethionate towards the promastigotes of the protozoan parasite Leishmaniainfantum is determined. The leishmanicidal activity of Pentamidine isethionate is 60 times higher after 72 h ofincubation than that of Cisplatin. Pentamidine isethionate induces a high

9、er 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 ofPentamidine isethionate to calf-thymus DNA (CT-DNA) induces conformational changes in the DNA double helix,consistent with a B-A transition.

10、 The interaction of Pentamidine isethionate with ubiquitin leads to a 6% increase inthe beta-sheet content of the protein2.Cell Viability Assay1Cell Line: WM9, DU145, C4-2, Hey, WM480, and A549 cellsConcentration: 0-10 g/mLIncubation Time: 6 daysResult: The growth of all six of the cell lines in cul

11、ture was inhibited in a concentration-dependent manner with complete growth inhibition of the cell lines occurring at 10g/mL.体内研究 Pentamidine (0.25 mg/mouse; intramuscular injection; every 2 days; for 4 weeks; athymic nude mice) treatmentmarkedly inhibits the growth of WM9 human melanoma tumors in n

12、ude mice1.Animal Model: Athymic nude mice (6 weeks old) injected with WM9 cells1Dosage: 0.25 mg/mouseAdministration: Intramuscular injection; every 2 days; for 4 weeksResult: Markedly inhibited the growth of WM9 human melanoma tumors in nude mice.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Molecules. 2020 A

13、pr 23;25(8). pii: E1980. Biochem Biophys Res Commun. 2019 Sep 17;517(2):221-226.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Sands M, et al. Pentamidine: a review. Rev Infect Dis. 1985 Sep-Oct;7(5):625-34.2. Pathak MK, et al. Pentamidine is an inhibitor of PRL pho

14、sphatases with anticancer activity. Mol Cancer Ther. 2002 Dec;1(14):1255-64.3. Nguewa, P.A., et al., Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400.4. David C. Bean, et al. Pentamidine: a drug to consider re-purposing in the targeted treatment of multi-drug resistant bacterial infections? J Lab PrecisMed 2017;2:49.McePdfH