1. Membrane Transporter/Ion Channel
  2. Ferroportin
  3. VIT-2763

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.

For research use only. We do not sell to patients.

VIT-2763 Chemical Structure

VIT-2763 Chemical Structure

CAS No. : 2095668-10-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1550 In-stock
100 mg USD 2400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE VIT-2763

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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)[1].
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[1].
VIT-2763 (100 nM) triggers ubiquitination and subsequent internalization and degradation of ferroportin[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Molecular Weight

408.43

Formula

C21H21FN6O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=COC(CCNCCC2=NC3=CC=CC=C3N2)=N1)NCC4=NC=CC=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (204.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4484 mL 12.2420 mL 24.4840 mL 61.2100 mL
5 mM 0.4897 mL 2.4484 mL 4.8968 mL 12.2420 mL
10 mM 0.2448 mL 1.2242 mL 2.4484 mL 6.1210 mL
15 mM 0.1632 mL 0.8161 mL 1.6323 mL 4.0807 mL
20 mM 0.1224 mL 0.6121 mL 1.2242 mL 3.0605 mL
25 mM 0.0979 mL 0.4897 mL 0.9794 mL 2.4484 mL
30 mM 0.0816 mL 0.4081 mL 0.8161 mL 2.0403 mL
40 mM 0.0612 mL 0.3061 mL 0.6121 mL 1.5303 mL
50 mM 0.0490 mL 0.2448 mL 0.4897 mL 1.2242 mL
60 mM 0.0408 mL 0.2040 mL 0.4081 mL 1.0202 mL
80 mM 0.0306 mL 0.1530 mL 0.3061 mL 0.7651 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6121 mL
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VIT-2763 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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VIT-2763
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