Deferoxamine mesylate (Deferoxamine B mesylate) 是一种铁螯合剂 (结合 Fe(III) 和许多其他金属阳离子)，被广泛用于减少铁在组织中的积累和沉积。Deferoxamine mesylate 可上调HIF-1α水平，具有较好的抗氧化活性，还能抗增殖和诱导癌细胞凋亡。Deferoxamine mesylate 可用于糖尿病、神经退行性疾病以及抗癌和抗 COVID-19 的研究。
| 生物活性 | Deferoxamine mesylate (Deferoxamine B mesylate) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine mesylate upregulatesHIF-1αlevels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induceapoptosisandautophagyincancercells. Deferoxamine mesylate can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19[1][2][3][4][5]. |
体外研究
(In Vitro) | Deferoxamine mesylate (1 mM; 16 h or 4 weeks) improves HIF-1α function under hypoxic and hyperglycemic conditions and decreases ROS in MEFs cells[1].
Deferoxamine mesylate (100 μM; 24 h) increases InsR expression and activity and also induces an increase in p-Akt/total Akt/PKB levels[2].
Deferoxamine mesylate (5, 10, 25, 50, 100 μM; 7 or 9 days) inhibits the proliferation of tumor-associated MSCs and bone marrow MSCs[3].
Deferoxamine mesylate (5, 10, 25, 50, 100 μM; 7 days) induces apoptosis of MSCs[3].
Deferoxamine mesylate (10 μM ; 3 days) influencs the expression of adhesion proteins on MSCs[3].
Deferoxamine mesylate (100 μM; 24 h) induces autophagy mediated by the level of HIF-1α in SH-SY5Y cells[4].
Western Blot Analysis[1] | Cell Line: | MEFs cells | | Concentration: | 1 mM | | Incubation Time: | 16 h (hypoxia condition); 4 weeks (hyperglycemic conditions) | | Result: | Significantly attenuated the hyperglycemia-associated increase in ROS levels under hypoxic high glucose conditions.
Notably increased normoxic HIF transactivation in MEFs under both high glucose and normal glucose conditions. |
Western Blot Analysis[2] | Cell Line: | HepG2 cells | | Concentration: | 100 μM | | Incubation Time: | 24 h | | Result: | Showed a twofold increase of InsR mRNA levels in cells.
Increased by twofold InsR binding activity at the half-maximal concentration of 1.1 nM. |
Cell Proliferation Assay[3] | Cell Line: | TAMSCs and BMMSCs (all isolated from Male C57BL/6J mice (8 week-old; EG-7 induced tumor model)) | | Concentration: | 5, 10, 25, 50, 100 μM | | Incubation Time: | 7 days (TAMSCs); 9 days (BMMSCs) | | Result: | Inhibited the growth of TAMSCs and BMMSCs, and most cells are died at day 7 or 9 when exposed to 50 and 100 μM dose. |
Apoptosis Analysis[3] | Cell Line: | TAMSCs, BMMSCs | | Concentration: | 5, 10, 25, 50, 100 μM | | Incubation Time: | 7 days | | Result: | Exhibited proapoptotic effect on TAMSCs and BMMSCs cells. |
Western Blot Analysis[3] | Cell Line: | TAMSCs, BMMSCs | | Concentration: | 10 μM | | Incubation Time: | 3 days | | Result: | Remarkably decreased VCAM-1 expression in both TAMSCs and BMMSCs. |
Cell Autophagy Assay[4] | Cell Line: | SH-SY5Y cells | | Concentration: | 100 μM | | Incubation Time: | 24 h | | Result: | Increased the ratio of LC3-II/I, an indicator of autophagy, which effects were blocked when autophagy-related geneBeclin 1was suppressed byBeclin 1siRNA transfection.
Caused a time and dose-dependent increase of HIF-1a, accompanied by the induction of autophagy. |
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体内研究
(In Vivo) | Deferoxamine mesylate (560.68 mg/per; drip-on; once daily for 21 days) enhances wound healing and increases neovascularization in aged or diabetic mice[1].
Deferoxamine mesylate (200 mg/kg; i.p.; daily for 2 weeks) results in HIF-1α stabilization and increases glucose uptake, hepatic InsR expression, and signaling in vivo[2].
| Animal Model: | Aged (21-month-old) and diabetic (12-week-old) C57BL/6J mice (excisional wound model)[1]. | | Dosage: | 560.68 mg/per (10 uL of 1 mM) | | Administration: | Drip-on; once daily for 21 days. | | Result: | Displayed significantly accelerated healing and increased neovascularization in both aged and diabetic mice model. |
| Animal Model: | Male Sprague-Dawley rats (180-200 g)[2]. | | Dosage: | 200 mg/kg | | Administration: | Intraperitoneal injection; daily for 2 weeks. | | Result: | Significantly increased hepatic HIF-1α protein levels, InsR protein levels, as well as Akt/PKB and activated Akt/PKB were significantly higher in the liver. |
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| 中文名称 | 甲磺酸去铁胺；去铁胺甲磺酸酯；甲磺酸去铁敏；甲磺酸除铁灵 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 250 mg/mL(380.64 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.5226 mL | 7.6128 mL | 15.2256 mL | | 5 mM | 0.3045 mL | 1.5226 mL | 3.0451 mL | | 10 mM | 0.1523 mL | 0.7613 mL | 1.5226 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: 5.56 mg/mL (8.47 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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