Exerenibart
REGN7999 is a monoclonal antibody that inhibits TMPRSS6. REGN7999 inhibits TMPRSS6 activity, preventing Hemojuvelin (HJV) lysis, thereby enhancing BMP6-HJV signaling and increasing serum hepcidin. REGN7999 ameliorates iron overload and impaired erythropoiesis in a β-thalassemia mouse model by inhibiting TMPRSS6 activity. REGN7999 is indicated for research in β-thalassemia.
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- No. CAS: 2996101-49-4
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Almacenamiento:
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Actividad biológica
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Actividad biológica
Human
TMPRSS6
REGN7999 blocks human and mouse TMPRSS6 activity, with IC50s of 0.68, 16 nM, and prevents HJV cleavage in overexpressing HJV and TMPRSS6 HEK293 cells[2].
REGN7999 bounds TMPRSS6 and inhibits TMPRSS6 activity across species, reduces proteolytic activity of human reference and variant TMPRSS6, cynomolgus monkey TMPRSS6, and mouse TMPRSS6[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
REGN7999 (5 mg/kg, s.c., once) increases serum hepcidin and decreases in serum iron in C57BL/6 mice model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hbbth3/+ mice model[1][2]
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Dosage:10 mg/kg
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Administration:s.c., once a week, 12 weeks
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Result:Reduced liver iron (~50% reduction compared to the isotype-treated group), improved RBC health as determined by reduced annexin V staining and RBC turnover, extend the RBC life span.
Elevated serum hepcidin and hepatic HAMP1 expression, did not increase markers of liver damage.
Reduced spleen weights to WT levels, displayed normalized reticulocyte numbers, blunted the increase in oxidative stress in blood and spleens, reduced bilirubin levels and lower expression levels of hepatic Hmox1, improved anaerobic capacity, increased bone mineral density.
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Animal Model:C57BL/6 mice model[2]
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Dosage:5 mg/kg
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Administration:s.c., once
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Result:Increased serum hepcidin, and decreased in serum iron, led to a significant drop of transferrin saturation and serum iron in the first 24 hours.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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No. CAS 2996101-49-4
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SMILES
N/A
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Synonyms
REGN7999
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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