VIT-2763 |
Katalog-Nr.GC60382
One-Click Copy Product Info
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VIT-2763, ein oraler Ferroportin-Inhibitor, hemmt die Bindung von Hepcidin an Ferroportin und blockiert den Eisenausfluss.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2095668-10-1
Sample solution is provided at 25 µL, 10mM.
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VIT-2763 is an oral, small-molecule ferroportin inhibitor that reduces serum iron and transferrin saturation (TSAT) levels [1]. VIT-2763 competes with hepcidin for binding to ferroportin, displacing hepcidin bound to recombinant ferroportin, and reducing cellular iron efflux [2]. VIT-2763 has been widely used to reduce the amount of early erythroid precursors in the bone marrow and spleen, and increase the number of mature erythrocytes [3].
In vitro, VIT-2763 treatment for 15 minutes significantly inhibited the internalization of fluorescently labeled hepcidin (TMR-hepcidin) in J774 cells, with an IC50 value of 9nM[4].
In vivo, VIT-2763 treatment via oral administration at a dose of 30mg/kg/day for 7 days exacerbated Plasmodium infection in mice and enhanced inflammatory responses and liver injury[5]. Daily administration of water containing 1mg/ml VIT-2763 for 10 weeks significantly reduced the spleen enlargement and alleviated systemic lupus nephritis in MRL/lpr mice[6]. Oral administration of VIT-2763 at a dose of 30mg/kg/day for 3 weeks improved anemia and erythropoiesis in a mouse model of β-thalassemia[7]. Daily intragastric administration of a 240mg/kg dose of VIT-2763 was carried out for 3 months, which significantly alleviated the cardiopulmonary dysfunction in the subchronic moderate hypoxia model of Berkeley SCD mice[8].
References:
[1] Kattamis A, Taher A, Viprakasit V, et al. Safety and pharmacodynamics of the ferroportin inhibitor vamifeport in patients with non-transfusion-dependent β-thalassemia: results from a randomized phase 2a study[J]. Orphanet Journal of Rare Diseases, 2025, 20(1): 608.
[2] Porter J, Taher A, Viprakasit V, et al. Oral ferroportin inhibitor vamifeport for improving iron homeostasis and erythropoiesis in β-thalassemia: current evidence and future clinical development[J]. Expert Review of Hematology, 2021, 14(7): 633-644.
[3] Pilo F, Angelucci E. Vamifeport: monography of the first oral ferroportin inhibitor[J]. Journal of Clinical Medicine, 2024, 13(18): 5524.
[4] Manolova V, Nyffenegger N, Flace A, et al. Oral ferroportin inhibitor ameliorates ineffective erythropoiesis in a model of β-thalassemia[J]. The Journal of clinical investigation, 2020, 130(1): 491-506.
[5] Zeydabadinejad S, Theis B F, Park J S, et al. Pharmacologic Inhibition of Erythrocyte Ferroportin Expression Exacerbates Plasmodium Infection[J]. Microorganisms, 2025, 13(8): 1859.
[6] Katikaneni D, Arekar T, Al-Hraki L, et al. Vamifeport, a clinical stage oral ferroportin inhibitor, alleviates murine lupus nephritis: A pilot study[J]. Clinical Immunology, 2026: 110699.
[7] Nyffenegger N, Flace A, Doucerain C, et al. The oral ferroportin inhibitor VIT-2763 improves erythropoiesis without interfering with iron chelation therapy in a mouse model of β-thalassemia[J]. International journal of molecular sciences, 2021, 22(2): 873.
[8] Lucero M J, Setua S, Thangaraju K, et al. Ferroportin inhibition attenuates pulmonary hypertension in hypoxic sickle cell disease mice[J]. Blood Advances, 2026, 10(9): 3229-3242.
| Cell experiment [1]: | |
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Cell lines |
J774 cells |
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Preparation Method |
J774 cells were cultured at 8×105 cells/ml in DMEM medium supplemented with fetal bovine serum, penicillin-streptomycin in 96-well plates at 37°C with 5% CO2 and 95% saturated atmospheric humidity. After overnight incubation, cells were washed, and serial dilutions of VIT-2763 (0, 0.001, 0.01, 0.1, 1, and 10µM) were added in triplicate. J774 cells were preincubated with VIT-2763 for 15 minutes before the addition of TMR-hepcidin at 25nM. Cells were incubated for 2 hours, and Hoechst 33342 dye was added to a final concentration of 0.5μg/ml. Cells were washed with PBS and fixed using 5.3% paraformaldehyde for 15 minutes. The fluorescence images were acquired. |
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Reaction Conditions |
0, 0.001, 0.01, 0.1, 1, and 10µM; 15min |
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Applications |
VIT-2763 treatment significantly inhibited the internalization of TMR-hepcidin within J774 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Hbbth3/+ mice |
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Preparation Method |
Hbbth3/+ mice (11 weeks old) were fed a low-iron diet (Fe=11mg/kg) and once daily with 120mg/kg of VIT-2763, or vehicles, for 3 weeks under a 12h light and 12h dark cycle at a temperature of 25°C and humidity of 50%±10%, with free water. The anemia and erythropoiesis were analyzed. Dosing was performed in the dark phase of the facility room, corresponding to the active period of rodents. Wild-type C57BL/6 mice dosed with vehicle served as controls. The anemia state and erythropoiesis in mice were analyzed. |
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Dosage form |
120mg/kg/day for 3 weeks; p.o. |
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Applications |
VIT-2763 treatment ameliorated anemia and ineffective erythropoiesis in Hbbth3/+ mice. |
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References: |
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| Cas No. | 2095668-10-1 | SDF | |
| Canonical SMILES | O=C(C1=COC(CCNCCC2=NC3=CC=CC=C3N2)=N1)NCC4=NC=CC=C4F | ||
| Formula | C21H21FN6O2 | M.Wt | 408.43 |
| Löslichkeit | Storage | -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4484 mL | 12.242 mL | 24.484 mL |
| 5 mM | 489.7 μL | 2.4484 mL | 4.8968 mL |
| 10 mM | 244.8 μL | 1.2242 mL | 2.4484 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: Viscous solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)