Deferidone

Research use only, not for human use.

Deferiprone is an oral iron chelator used as a second line agent in thalassemia syndromes when iron overload from blood transfusions occurs.

Deferiprone is an oral iron chelator used as a second line agent in thalassemia syndromes when iron overload from blood transfusions occurs. Thalassemias are a type of hereditary anaemia due a defect in the production of hemoglobin. As a result, erythropoiesis, the production of new red blood cells, is impaired. FDA approved on October 14, 2011.

Cell Viability Assay Cell Line:TRAMP-C2, Myc-CaP, and 22rv1 cells Concentration:0, 16, 30, 66, 100, 160, 300, 660 μM Incubation Time:48 h, 72 h Result:Showed a cytostatic effect in three cell lines with an IC50 and IC90 values of about 50 and 100 μM, respectively.Cell Migration Assay Cell Line:TRAMP-C2, Myc-CaP, and 22rv1 cells Concentration:100 μM Incubation Time:0 to 30 h for TRAMP-C2, and Myc-CaP; 0 to 192 h for 22rv1 Result:Inhibited cell migration starting at different time points for each cell line, ranging from 12 h in TRAMP-C2 cell to 48 h in 22rv1 cells, and 30 h in Myc-CaP cells.Western Blot Analysis Cell Line:TRAMP-C2, Myc-CaP, and 22rv1 cells Concentration:100 μM Incubation Time:24 h Result:Reduced the expression of m-Acon, by 2-fold in Myc-CaP and 22 rv1 cells and decreased by 79% in TRAMP-C2 cells.

Animal Model:The rTg(tauP301L)4510 mouse model of tauopathy.Dosage:100 mg/kg/daily, 4 weeksAdministration:Intragastric administration (i.g.)Result:Improved Y-maze and open field performance, and decreased 28% iron levels in brain, and reduced AT8-labeled p-tau within the hippocampus in transgenic tau mice.Animal Model:Cisplatin(HY-17394)-induced rat acute renal failure model Dosage:50, 100, 200 mg/kg, 5-10 dayAdministration:Oral administrationResult:Reduced the creatinine, BUN, malondialdehyde, iron concentrations, and theamounts of TfR, and indreased the levels of HIF-1a and related anti-apoptotic genes expression in Cisplatin (HY-17394)-injected animals.Animal Model:Aluminium-linked apoptosis in rat hippocampus model (Alzheimer’s disease model) Dosage:13.82, 27.64 mg/kg/d, 4 week Administration:Intragastric administration lasting 6 days with 1 day interval per week Result:Decreased the apoptosis and the expression of Caspase-3 and Bax, and increased the expression of Bcl-2 in Aluminium-linked apoptosis in rat hippocampus.

CGP 37391 | DN 18001AF

Metabolic Enzyme/Protease

Other Targets

iron| UGT1-6

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30652-11-0

139.15

C7H9NO2

>98% (HPLC)

Water: 1 mg/mL (7.18 mM)

O=C1C(O)=C(C)N(C)C=C1

3-hydroxy-1,2-dimethylpyridin-4(1H)-one

(-20℃)

With Ice Pack

≥ 2 years