新闻资讯

新闻中心
首页>新闻资讯>新闻中心

2023-03-22 17:50:52

Deferoxamine mesylate (Synonyms: 甲磺酸去铁胺; Desferrioxamine B mesylate; DFOM)

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。

Deferoxamine mesylate Chemical Structure




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 upregulates HIF-1α levels with good antioxidant activity. Deferoxamine mesylate also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line:MEFs cellsConcentration:1 mMIncubation 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.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT NumberSponsorConditionStart DatePhaseNCT00600938Novartis Pharmaceuticals|NovartisTransfusional Iron Overload|Transfusional HemosiderosisNovember 2007Phase 2NCT03137966Karolinska University HospitalDiabetic Foot UlcerDecember 30, 2022Phase 2NCT01254227Novartis Pharmaceuticals|NovartisCardiac Iron OverloadJanuary 2011Phase 2

分子量

656.79

性状

Solid

Formula

C26H52N6O11S

CAS 号

138-14-7

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


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

浓度溶剂体积质量1 mg5 mg10 mg1 mM1.5226 mL7.6128 mL15.2256 mL5 mM0.3045 mL1.5226 mL3.0451 mL10 mM0.1523 mL0.7613 mL1.5226 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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

  • 请依序添加每种溶剂: PBS

    Solubility: 5.56 mg/mL (8.47 mM); Clear solution; Need ultrasonic


参考文献


推荐新闻