VIT-2763 - 10mM in DMSO , CAS No.2095668-10-1

CAS: 2095668-10-1 Cat. No.: V655303 Formula: C₂₁H₂₁FN₆O₂ Peso molecolare: 408.43 PubChem CID: 129052159

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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.

In Vitro

VIT-2763 dose dependently reduces the fluorescence polarization signal, indicating that VIT-2763 displaces TMR-hepcidin from ferroportin (IC 50 of 24 ± 13 nM). VIT-2763 induces BLA reporter gene activity with an average EC 50 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. MCE 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.

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 . MCE 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.

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

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.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Nomi e identificatori

• Isomeri SMILES: C1=CC=C2C(=C1)NC(=N2)CCNCCC3=NC(=CO3)C(=O)NCC4=C(C=CC=N4)F
• CAS alternativo: 2095668-10-1
• PubChem CID: 129052159
• Termini MeSH: VIT-2763
• Peso molecolare: 408.43

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2095668-10-1, the molecular formula is C21H21FN6O2, and the molecular weight is 408.43 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.