Deferidone

SKU: orb1225357

Description

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.

Key Properties

• CAS Number: 30652-11-0
• MW: 139.15
• Purity: >98% (HPLC)
• Formula: C₇H₉NO₂
• SMILES: O=C1C(O)=C(C)N(C)C=C1
• Target: iron| UGT1-6
• Solubility: Water: 1 mg/mL (7.18 mM)

Bioactivity

• In Vivo:
  Animal model: The rTg(tauP301L)4510 mouse model of tauopathy. Dosage: 100 mg/kg/daily, 4 weeks. Administration: 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 day. Administration: Oral administration. Result: 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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CGP 37391 | DN 18001AF

Quick Database Links

Gene Symbol

iron| UGT1-6