VIT-2763 

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^[1].

VIT-2763 剂量依赖性地降低荧光偏振信号，表明 VIT-2763 从膜铁转运蛋白中取代了 TMR-铁调素 (IC₅₀ 为 24 nM)^[1]。
VIT-2763 诱导 BLA 报告基因活性，平均 EC₅₀ 为 140 nM，这是由于 HEK293 细胞中铁输出受阻导致细胞内铁浓度升高所致^[1]。
VIT-2763 (100 nM) 触发泛素化以及随后的膜铁转运蛋白内化和降解^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

VIT-2763 (30，100 mg/kg，每日两次口服，共 36 天) 可降低 Hbb^th3/+ 小鼠的血清铁含量并防止肝脏铁负荷^[1]。
VIT-2763 不会改变肝脏总铁含量^[1]。
VIT-2763 (30，100 mg/kg，每日两次口服，共 36 天) 可显著纠正 Hbb^th3/+ 小鼠的贫血并改善红细胞参数。VIT-2763 将 Hbb^th3/+ 小鼠中 ROS 阳性红细胞的百分比从 67% 降低至 30%^[1]。
VIT-2763 可减少 Hbb^th3/+ 小鼠中红细胞的凋亡并延长其寿命^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

408.43

C₂₁H₂₁FN₆O₂

2095668-10-1

固体

Off-white to light yellow

Room temperature in continental US; may vary elsewhere.

• [1]. Vania Manolova, et al. Oral Ferroportin Inhibitor Ameliorates Ineffective Erythropoiesis in a Model of β-Thalassemia. J Clin Invest. 2019 Dec 9;130(1):491-506.  [Content Brief]