产品
编 号：F620941
分子式：C21H21FN6O2
分子量：408.43
分子式：C21H21FN6O2
分子量：408.43
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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结构图
CAS No: 2095668-10-1
产品详情
生物活性：
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.
体内研究：
VIT-2763 (30, 100 mg/kg, orally twice daily for 36 days) decreases serum iron and prevented liver iron loading in Hbbth3/+ mice.VIT-2763 did not change the total liver iron.VIT-2763 (30, 100 mg/kg, orally twice daily for 36 days) significantly corrects anemia and improved RBC parameters in Hbbth3/+ mice. VIT-2763 decreases the percentage of ROS-positive RBCs in Hbbth3/+ mice from 67% to 30%.VIT-2763 decreases apoptosis and extends the life span of RBCs in Hbbth3/+ mice.Animal Model:Hbbth3/+ mice.
Dosage:30, 100 mg/kg.
Administration:Orally twice daily for 36 days.
Result:Significantly decreased serum iron levels by 77% (30 mg/kg) and 84% (100 mg/kg),Significantly increased Hb levels (as of day 8 of treatment), RBC counts, mean corpuscular Hb concentration (MCHC), and significantly lowered reticulocyte counts, mean corpuscular Hb (MCH), mean corpuscular volume (MCV), and RBC distribution width (RDW) in Hbbth3/+ mice, as compared with the Hbbth3/+ vehicle group.
体外研究：
VIT-2763 dose dependently reduces the fluorescence polarization signal, indicating that VIT-2763 displaces TMR-hepcidin from ferroportin (IC50 of 24 ± 13 nM).VIT-2763 induces BLA reporter gene activity with an average EC50 of 140 ± 50 nM, as a consequence of increasing intracellular iron concentrations caused by blocked iron export in HEK293 cells.VIT-2763 (100 nM) triggers ubiquitination and subsequent internalization and degradation of ferroportin.
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.
体内研究：
VIT-2763 (30, 100 mg/kg, orally twice daily for 36 days) decreases serum iron and prevented liver iron loading in Hbbth3/+ mice.VIT-2763 did not change the total liver iron.VIT-2763 (30, 100 mg/kg, orally twice daily for 36 days) significantly corrects anemia and improved RBC parameters in Hbbth3/+ mice. VIT-2763 decreases the percentage of ROS-positive RBCs in Hbbth3/+ mice from 67% to 30%.VIT-2763 decreases apoptosis and extends the life span of RBCs in Hbbth3/+ mice.Animal Model:Hbbth3/+ mice.
Dosage:30, 100 mg/kg.
Administration:Orally twice daily for 36 days.
Result:Significantly decreased serum iron levels by 77% (30 mg/kg) and 84% (100 mg/kg),Significantly increased Hb levels (as of day 8 of treatment), RBC counts, mean corpuscular Hb concentration (MCHC), and significantly lowered reticulocyte counts, mean corpuscular Hb (MCH), mean corpuscular volume (MCV), and RBC distribution width (RDW) in Hbbth3/+ mice, as compared with the Hbbth3/+ vehicle group.
体外研究：
VIT-2763 dose dependently reduces the fluorescence polarization signal, indicating that VIT-2763 displaces TMR-hepcidin from ferroportin (IC50 of 24 ± 13 nM).VIT-2763 induces BLA reporter gene activity with an average EC50 of 140 ± 50 nM, as a consequence of increasing intracellular iron concentrations caused by blocked iron export in HEK293 cells.VIT-2763 (100 nM) triggers ubiquitination and subsequent internalization and degradation of ferroportin.
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