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VIT-2763

目录号: PL11778 纯度: ≥98%

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。

CAS No. :2095668-10-1

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中文名称	VIT-2763
英文名称	VIT-2763
英文别名	FUF66UD0KR;Vamifeport;Vamifeport [INN];vamifeport (proposed INN);GTPL11183;VIT2763;N1C(=NC2=C1C=CC=C2)CCNCCC=1OC=C(N=1)C(=O)NCC1=NC=CC=C1F;2-(2-((2-(1H-Benzimidazol-2-yl)ethyl)amino)ethyl)-N-((3-fluoropyridin-2-yl)methyl)-1,3-oxazole-4-carboxamide;2-[2-[2-(1H-benzimidazol-2-yl)ethylamino]ethyl]-N-[(3-fluoropyridin-2-yl)methyl]-1,3-oxazole-4-carboxamide;4-Oxazolecarboxamide, 2-(2-((2-(1H-benzimidazol-2-yl)ethyl)amino)ethyl;Unii-fuf66UD0KR;VIT-2763
Cas No.	2095668-10-1
分子式	C₂₁H₂₁FN₆O₂
分子量	408.43
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	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。

产品详情

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。

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.

性状

Solid

体外研究(In Vitro)

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

体内研究(In Vivo)

VIT-2763 (30, 100 mg/kg, orally twice daily for 36 days) decreases serum iron and prevented liver iron loading in Hbb 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 Hbb mice. VIT-2763 decreases the percentage of ROS-positive RBCs in Hbb mice from 67% to 30%.
VIT-2763 decreases apoptosis and extends the life span of RBCs in Hbb mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (306.05 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

VIT-2763

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