VIT-2763|cas:2095668-10-1|西域试剂

VIT-2763,99.87%

产品编号：Bellancom-112220| CAS NO：2095668-10-1| 分子式：C₂₁H₂₁FN₆O₂| 分子量：408.43

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-112220	￥3500.00	杭州北京（现货）
Bellancom-112220	￥5500.00	杭州北京（现货）
Bellancom-112220	￥15500.00	杭州北京（现货）
Bellancom-112220	￥24000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

VIT-2763

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 oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.

体外研究

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.

西域 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.

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.
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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。