噴他脒羥乙磺酸鹽作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetPentamidine isethionateCat. No.: HY-B0537BCAS No.: 140-64-7分式: CHNOS分量: 592.68作靶點: Parasite; Fungal; Phosphatase; Bacterial作通路: Anti-infection; Metabolic Enzyme/Protease儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實驗 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制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 m

3、onths; -20C, 1 month (protect from light)。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80

4、45% salineSolubility: 2.5 mg/mL (4.22 mM); Clear solution此案可獲得 2.5 mg/mL (4.22 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.22 mM); Clear solu

5、tion此案可獲得 2.5 mg/mL (4.22 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.22 mM); Clear solution此案可獲得 2.5 mg/mL (4.22 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L

6、25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Pentamidine isethionate (MP-601205 isethionate)種抗微物劑，會擾 DNA 的物合成。Pentamidineisethionate 抑制寄 Leishmania infantum，IC50 為 2.5 M。Pentamidine isethionate 種有效的選擇性蛋酪氨酸磷酸酶 (PTPases) 和再肝磷酸酶 (PRL) 抑制劑。Pentamidine isethionate 可于岡亞錐病，抗銻利什曼病和卡肺孢肺炎的研究。

7、抗腫瘤活性，抗菌活性。IC & Target IC50: 2.5 M (Leishmania infantum)2Protein tyrosine phosphatases (PTPases)1Phosphatase of regenerating liver (PRL)1體外研究 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.體內(nèi)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戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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