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2095668-10-1

2095668-10-1 Structure

2095668-10-1 Structure
IdentificationBack Directory
[Name]

4-Oxazolecarboxamide, 2-[2-[[2-(1H-benzimidazol-2-yl)ethyl]amino]ethyl]-N-[(3-fluoro-2-pyridinyl)methyl]-
[CAS]

2095668-10-1
[Synonyms]

VIT-2763
4-Oxazolecarboxamide, 2-[2-[[2-(1H-benzimidazol-2-yl)ethyl]amino]ethyl]-N-[(3-fluoro-2-pyridinyl)methyl]-
[Molecular Formula]

C21H21FN6O2
[MOL File]

2095668-10-1.mol
[Molecular Weight]

408.43
Chemical PropertiesBack Directory
[Boiling point ]

727.8±60.0 °C(Predicted)
[density ]

1.339±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

11.87±0.46(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Uses]

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 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].

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.
[References]

[1] Vania Manolova, et al. Oral Ferroportin Inhibitor Ameliorates Ineffective Erythropoiesis in a Model of β-Thalassemia. J Clin Invest. 2019 Dec 9;130(1):491-506. DOI:10.1172/JCI129382
Spectrum DetailBack Directory
[Spectrum Detail]

4-Oxazolecarboxamide, 2-[2-[[2-(1H-benzimidazol-2-yl)ethyl]amino]ethyl]-N-[(3-fluoro-2-pyridinyl)methyl]-(2095668-10-1)1HNMR
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