Deferoxamine mesylate
(Synonyms: 甲磺酸去铁胺; Desferrioxamine B mesylate; DFOM) 目录号 : GC13554
Deferoxamine mesylate 是一种通过形成稳定的复合物来螯合铁的药物，该复合物可防止铁进入进一步的化学反应，并用于治疗输血依赖性贫血患者的慢性铁过载。
Cas No.:138-14-7
Sample solution is provided at 25 µL, 10mM.
Deferoxamine mesylate is a drug that chelates iron by forming a stable complex that prevents the iron from entering into further chemical reactions, and is used for the treatment of chronic iron overload in patients with transfusion-dependent anemias[1,2].
Deferoxamine mesylate (260μM) is directly toxic on RPE cells, its toxicity depending on p38[1]. Deferoxamine mesylate administration resulted in reduced cytotoxicity and ROS generation by Fe(Salen) in Rabbit squamous cell carcinoma (VX2) cells, human glioblastoma malignant glioma cells (YKG)OVK18, and human ovarian carcinoma cells[3]. Deferoxamine mesylate (30μM) significantly inhibits the growth of human hepatocellular carcinoma and hepatoblastoma cell lines[4].
Deferoxamine mesylate enhances urinary iron elimination and decreases hepatic iron accumulation after blood transfusion in foals[2]. Deferoxamine mesylate (25mg/kg, intravenous injection) reduced the onset of Fe (Salen) (25mg/kg)-induced acute liver and renal dysfunction. Deferoxamine mesylate (300mg/kg) improves survival rate after systematic injection of a fatal dose of Fe (Salen) (200mg/kg) in Male ICR[3]. Use of deferoxamine mesylate in bone defects promotes vascularization and osteogenesis in the defect area, and maintains the protein activity of HIF-1α temporarily[5]. Deferoxamine mesylate can ameliorate tissue ischemia-reperfusion injury. Deferoxamine mesylate preconditioning protected pancreatic tissue in orthotopic liver autotransplantation in rats[6].
References:
[1] Klettner A, Koinzer S, et al. Deferoxamine mesylate is toxic for retinal pigment epithelium cells in vitro, and its toxicity is mediated by p38. Cutan Ocul Toxicol. 2010;29(2):122-129.
[2] Elfenbein JR, Giguère S, et al. The effects of deferoxamine mesylate on iron elimination after blood transfusion in neonatal foals. J Vet Intern Med. 2010;24(6):1475-1482.
[3] Umemura M, Kim JH, et al. The iron chelating agent, deferoxamine detoxifies Fe(Salen)-induced cytotoxicity. J Pharmacol Sci. 2017;134(4):203-210.
[4] Tabor E, Kim CM. Inhibition of human hepatocellular carcinoma and hepatoblastoma cell lines by deferoxamine. J Med Virol. 1991;34(1):45-50.
[5]DU WY, Yang JW, et al. [Early constant observation of the effect of deferoxamine mesylate on improvement of vascularized bone regeneration in SD rat skull critical size defect model]. Beijing Da Xue Xue Bao Yi Xue Ban. 2021 Dec 18;53(6):1171-1177. Chinese.
[6]Li Y, Zhang PJ, et al. Protective effects of deferoxamine mesylate preconditioning on pancreatic tissue in orthotopic liver autotransplantation in rats. Transplant Proc. 2011;43(5):1450-1455.
Deferoxamine mesylate 是一种通过形成稳定的复合物来螯合铁的药物，该复合物可防止铁进入进一步的化学反应，并用于治疗输血依赖性贫血患者的慢性铁过载[1, 2]。
Deferoxamine mesylate (260μM) 对 RPE 细胞有直接毒性，其毒性取决于 p38[1]。施用甲磺酸去铁胺可降低兔鳞状细胞癌 (VX2) 细胞、人胶质母细胞瘤恶性胶质瘤细胞 (YKG)OVK18 和人卵巢癌细胞中 Fe(Salen) 的细胞毒性和 ROS 生成[3] 。 Deferoxamine mesylate (30μM)显着抑制人肝细胞癌和肝母细胞瘤细胞系的生长[4]。
甲磺酸去铁胺增强马驹输血后尿液铁的消除并减少肝脏铁的积累[2]。 Deferoxamine mesylate (25mg/kg, 静脉注射)减少了Fe (Salen) (25mg/kg)诱导的急性肝肾功能障碍的发生。甲磺酸去铁胺 (300mg/kg) 在男性 ICR[3] 中系统注射致命剂量的 Fe (Salen) (200mg/kg) 后提高了存活率。甲磺酸去铁胺在骨缺损中的应用促进了缺损区域的血管形成和成骨，并暂时维持了HIF-1α的蛋白活性[5]。 Deferoxamine mesylate 可以改善组织缺血再灌注损伤。甲磺酸去铁胺预处理对大鼠原位自体肝移植胰腺组织的保护作用[6]。
| Cell experiment [1]: | |
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Cell lines |
RPE cells, 4 or 24h |
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Preparation Method |
Subconfluent RPE cells were stimulated for 4 hours or 24 hours with 0µM, 100µM, 260µM, or 500µM of deferoxamine mesylate suspended in sterile distilled water. |
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Reaction Conditions |
0µM, 100µM, 260µM, or 500µM deferoxamine mesylate |
|
Applications |
Deferoxamine mesylate induces significant cell death compared with untreated controls in the RPE cells when treated for 4 hours or 24 hours with 260µM and 500µM, but not when treated with 100µM, of deferoxamine. |
| Animal experiment [2]: | |
|
Animal models |
Male Sprague-Dawley rats, 180-200g |
|
Preparation Method |
Rats were either iron depleted by daily injections of 200mg/kg deferoxamine mesylate (Novartis)37 or submitted to injections of solvent (0.9% saline), for 2 weeks. |
|
Dosage form |
200mg/kg deferoxamine mesylate |
|
Applications |
Iron depletion by deferoxamine mesylate affects glucose metabolism inducing glucose uptake and utilization and increasing InsR binding activity and signaling, and that the mechanism is associated with HIF-1 stabilization and requires the presence of HIF-1/ARNT. |
|
References: [1]. Klettner A, Koinzer S, et al. Deferoxamine mesylate is toxic for retinal pigment epithelium cells in vitro, and its toxicity is mediated by p38. Cutan Ocul Toxicol. 2010;29(2):122-129. [2]. Dongiovanni P, Valenti L, et al. Iron depletion by deferoxamine up-regulates glucose uptake and insulin signaling in hepatoma cells and in rat liver. Am J Pathol. 2008;172(3):738-747. |
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| Cas No. | 138-14-7 | SDF | |
| 别名 | 甲磺酸去铁胺; Desferrioxamine B mesylate; DFOM | ||
| 化学名 | (Z)-4-((5-aminopentyl)(hydroxy)amino)-N-(5-((Z)-N,4-dihydroxy-4-((5-(N-hydroxyacetamido)pentyl)imino)butanamido)pentyl)-4-oxobutanimidic acid compound with methanesulfonic acid (1:1) | ||
| Canonical SMILES | CC(N(O)CCCCC/N=C(O)/CCC(N(O)CCCCC/N=C(O)/CCC(N(O)CCCCCN)=O)=O)=O.CS(O)(=O)=O | ||
| 分子式 | C26H52N6O11S | 分子量 | 656.79 |
| 溶解度 | ≥ 65.7mg/mL in Water | 储存条件 | Store at -20°C,protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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