Deferoxamine mesylate
|
Katalog-Nr.GC13554 |
Deferoxamine mesylate ist ein Medikament, das Eisen durch die Bildung eines stabilen Komplexes chelatisiert, wodurch das Eisen daran gehindert wird, in weitere chemische Reaktionen einzutreten. Es wird zur Behandlung von chronischer Eisenüberladung bei Patienten mit transfusionsabhängigen Anämien eingesetzt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 138-14-7
Sample solution is provided at 25 µL, 10mM.
Deferoxamine mesylate ist ein Medikament, das Eisen durch die Bildung eines stabilen Komplexes chelatisiert, wodurch das Eisen daran gehindert wird, in weitere chemische Reaktionen einzutreten. Es wird zur Behandlung von chronischer Eisenüberladung bei Patienten mit transfusionsabhängigen Anämien eingesetzt[1,2].
Deferoxamine mesylate (260μM) ist direkt toxisch für RPE-Zellen, wobei seine Toxizität von p38 abhängt[1]. Die Verabreichung von Deferoxamine mesylate führte zu einer reduzierten Zytotoxizität und ROS-Generierung durch Fe(Salen) in Kaninchen-Plattenepithelkarzinomzellen (VX2), menschlichen Glioblastom-Malignomzellen (YKG) OVK18 und menschlichen Ovarialkarzinomzellen[3]. Deferoxamine mesylate (30μM) hemmt signifikant das Wachstum von menschlichen hepatozellulären Karzinom- und Hepatoblastom-Zelllinien[4].
Deferoxamine mesylate fördert die Ausscheidung von Eisen im Urin und verringert die Ansammlung von Eisen in der Leber nach Bluttransfusionen bei Fohlen[2]. Deferoxamine mesylate (25mg/kg, intravenöse Injektion) reduzierte den Beginn der durch Fe (Salen) (25mg/kg) induzierten akuten Leber- und Nierenfunktionsstörung. Deferoxamine mesylate (300mg/kg) verbessert die Überlebensrate nach systemischer Injektion einer tödlichen Dosis von Fe (Salen) (200mg/kg) bei männlichen ICR-Mäusen[3]. Der Einsatz von Deferoxamine mesylate bei Knochendefekten fördert die Vaskularisierung und Osteogenese im Defektbereich und erhält vorübergehend die Proteinaktivität von HIF-1α[5]. Deferoxamine mesylate kann Gewebeischämie-Reperfusionsschäden mildern. Deferoxamine mesylate-Präkonditionierung schützte das Pankreasgewebe bei orthotoper Leberautotransplantation bei Ratten[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.
Cell experiment [1]: | |
Cell lines |
RPE cells, 4 or 24h |
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. |
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: |
Cas No. | 138-14-7 | SDF | |
Überlieferungen | Ba 33112, DFO, DFOM, DFX, NSC 644468 | ||
Chemical Name | (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 | ||
Formula | C26H52N6O11S | M.Wt | 656.79 |
Löslichkeit | ≥ 65.7mg/mL in Water | Storage | Store at -20°C,protect from light |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
![]() |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
DFO alleviates GLY-induced testosterone synthesis inhibition. (A) Representative blot and quantitative analysis of CYP11A1, HSD3B2, and StAR protein levels in cells (n = 3).
TM3 cells were pretreated with 100 μM DFO(GLPBIO) for 4 h before being cultured with 1 mM GLY for 24 h to perform experiments.
Sci Total Environ (2024): 169927. PMID: 38199345 IF: 9.8003 -
Related Biological Data
STAT6 expression and activation are upregulated along with ferroptosis induction during ALI H&E staining showed obvious inflammatory cell infiltration and thickened alveolar septum in the lung tissues of CS- and LPS-treated mice, which were attenuated by Ferr-1 and DFO (Supplementary Figs. S1E,F and S2E,F).
odels of CS + Ferr-1/DFO, mice were intraperitoneally injected with Ferr-1 (1.25 µmol/kg) or intranasal instilled with DFO (10 mg/kg)(GLPBIO) for 7 consecutive days after CS instillation.
Cell Death & Disease 13.6 (2022): 1-14. PMID: 35668064 IF: 8.4685 -
Related Biological Data
For the mInhibition of epithelium ferroptosis disturbs fibroblast activation.(A) Inhibition of Ferr-1 and DFO against CM-induced accumulation of lipid ROS are measured by BODIPY 581/591 C11 staining.
For the Ferr-1/DFO intervention, mice from the control (Ctrl) and CS groups were intraperitoneally injected with Ferr-1 (1.25 μmol/kg) once every two days until euthanized on the 56th day, or intranasally instilled with DFO (10 mg/kg)(GLPBIO) continuously for 56 days (n = 6 per group).
Ecotox Environ Safe 271 (2024): 115994. PMID: 38262094 IF: 6.7996 -
Related Biological Data
Erastin and sulfasalazine induce ferroptosis in Kasumi-1 and HL-60 cells. (C) Kasumi-1 and HL-60 cells treated with normal or 5μM erastin were cultured with Ferrostatin-1(2 μM), deferoxamine (100 μM), necrostatin-1 (10 μM), Z-VAD-FMK (10 μM) or chloroquine (25 μM) for 24 h, and cell viability was detected using the MTS assay.
Kasumi-1 and HL-60 cells treated with deferoxamine (100 μM) (GLPBIO)for 24 h, and cell viability was detected using the MTS assay.
Frontiers in Oncology 12 (2022): 930654. PMID: 36033479 IF: 4.7003
Average Rating: 5
(Based on Reviews and 7 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *