VIT-2763

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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。

CAS NO:

2095668-10-1

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 Hbb^th3/+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 Hbb^th3/+mice. VIT-2763 decreases the percentage of ROS-positive RBCs in Hbb^th3/+mice from 67% to 30%^[1].
VIT-2763 decreases apoptosis and extends the life span of RBCs in Hbb^th3/+mice^[1].

Animal Model:	Hbb^th3/+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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	2.4484 mL	12.2420 mL	24.4840 mL
5 mM	0.4897 mL	2.4484 mL	4.8968 mL
10 mM	0.2448 mL	1.2242 mL	2.4484 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。