1. Others
  2. Others
  3. VIT-2763

VIT-2763 

Cat. No.: HY-112220 Purity: 98.39%
Handling Instructions

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
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 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].

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].

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.

2095668-10-1

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
10 mM 0.2448 mL 1.2242 mL 2.4484 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

VIT-2763VIT2763VIT 2763Othersβ-thalassemiaROSubiquitinationironRBCInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
VIT-2763
Cat. No.:
HY-112220
Quantity:
MCE Japan Authorized Agent: