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Deferoxamine mesylate Verkauf (Synonyms: Ba 33112, DFO, DFOM, DFX, NSC 644468)

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.

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Deferoxamine mesylate Chemische Struktur

Cas No.: 138-14-7

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100mg
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500mg
86,00 $
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 6 publications

Description of Deferoxamine mesylate

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.

Protocol of Deferoxamine mesylate

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:
[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.

Chemical Properties of Deferoxamine mesylate

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.

Complete Stock Solution Preparation Table of Deferoxamine mesylate

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
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