Vamifeport

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VIT-2763 是具有口服活性的铁转运蛋白 (ferroportin) 的抑制剂，抑制hepcidin 与铁转运蛋白结合，阻滞铁外流。VIT-2763有用于地中海贫血症的潜力。

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.

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.Cell Viability Assay.Cell Line:J774 cells. Concentration:100 nM.Incubation Time:10, 20, 40, 60, or 120 minutes.Result:Induced ferroportin internalization and ubiquitination.

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.

——

Apoptosis

Ferroptosis

Ferroptosis

——

——

2095668-10-1

408.43

C21H21FN6O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 83.33 mg/mL (204.03 mM; 超声助溶 )

Fc1cccnc1CNC(=O)c1coc(CCNCCc2nc3ccccc3[nH]2)n1

——

(-20℃)

With Ice Pack

≥ 2 years