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VIT-2763
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VIT-2763图片
CAS NO:2095668-10-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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 oralferroportininhibitor, inhibits hepcidin binding toferroportinand blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia[1].

体外研究
(In Vitro)

VIT-2763 dose dependently reduces the fluorescence polarization signal, indicating that VIT-2763 displaces TMR-hepcidin from ferroportin (IC50of 24 ± 13 nM)[1].
VIT-2763 induces BLA reporter gene activity with an average EC50of 140 ± 50 nM, as a consequence of increasing intracellular iron concentrations caused by blocked iron export in HEK293 cells[1].
VIT-2763 (100 nM) triggers ubiquitination and subsequent internalization and degradation of ferroportin[1].

Cell Viability Assay[1].

Cell Line:J774 cells.
Concentration:100 nM.
Incubation Time:10, 20, 40, 60, or 120 minutes.
Result:Induced ferroportin internalization and ubiquitination.
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 Hbbth3/+mice[1].
VIT-2763 did not change the total liver iron[1].
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%[1].
VIT-2763 decreases apoptosis and extends the life span of RBCs in Hbbth3/+mice[1].

Animal Model:Hbbth3/+mice[1].
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.
Clinical Trial
分子量

408.43

性状

Solid

Formula

C21H21FN6O2

CAS 号

2095668-10-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL(306.05 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4484 mL12.2420 mL24.4840 mL
5 mM0.4897 mL2.4484 mL4.8968 mL
10 mM0.2448 mL1.2242 mL2.4484 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.09 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.09 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。