计算溶液所需的质量、体积或浓度。
Moligand™ 级 提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
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.
In Vitro
VIT-2763 dose dependently reduces the fluorescence polarization signal, indicating that VIT-2763 displaces TMR-hepcidin from ferroportin (IC 50 of 24 ± 13 nM). VIT-2763 induces BLA reporter gene activity with an average EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
In Vivo
VIT-2763 (30, 100 mg/kg, orally twice daily for 36 days) decreases serum iron and prevented liver iron loading in Hbb th3/+ 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 th3/+ mice. VIT-2763 decreases the percentage of ROS-positive RBCs in Hbb th3/+ mice from 67% to 30% . VIT-2763 decreases apoptosis and extends the life span of RBCs in Hbb th3/+ mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Hbb th3/+ 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.
Form:Solid
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 有机杂环化合物 |
| 类(Class) | 苯并咪唑类 |
| 亚类(Subclass) | 暂无 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 苯并咪唑类 |
| 其他上位类(Alternative Parents) | 2-杂芳基酰胺 芳烷基胺 2,4-二取代恶唑 吡啶及其衍生物 苯类化合物 芳基氟化物 咪唑类 杂芳族化合物 仲羧酸酰胺 氨基酸及其衍生物 氧环化合物 二烷基胺 氮杂环化合物 有机光子化合物 有机氧化合物 有机氟化物 有机氧化物 碳氢化合物衍生物 |
| 分子骨架(Molecular Framework) | 芳香族杂多环化合物 |
| 取代基(Substituents) | 2-异芳基甲酰胺 - 2,4-二取代-1,3-噁唑 - 氨基酸 - 氨基酸或其衍生物 - 芳烷基胺 - 芳香族杂多环化合物 - 芳基氟化物 - 芳基卤化物 - 氮杂环 - 吡唑 - 苯基化合物 - 苯并咪唑 - 羧酰胺基 - 羧酸衍生物 - 杂芳香族化合物 - 烃衍生物 - 咪唑 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机氟化物 - 有机卤化物 - 有机氮化合物 - 有机氧化合物 - 有机氮化合物 - 氧杂环 - 噁唑 - 吡啶 - 二级脂肪胺 - 醛基 - 醛基 |
| 描述(Description) | 该化合物属于苯并咪唑类有机化合物。这类化合物含有苯环与咪唑环(含氮原子、4个碳原子及两个双键的五元环)共轭的结构。 |
| 外部描述符(External Descriptors) | 暂无 |