Exerenibart
Based on 1 Customer Validation
Exerenibart (REGN7999) is a monoclonal antibody that inhibits TMPRSS6. Exerenibart inhibits TMPRSS6 activity, preventing Hemojuvelin (HJV) lysis, thereby enhancing BMP6-HJV signaling and increasing serum hepcidin. Exerenibart ameliorates iron overload and impaired erythropoiesis in a β-thalassemia mouse model by inhibiting TMPRSS6 activity. Exerenibart is indicated for research in β-thalassemia.
For research use only. We do not sell to patients.
- Purity : 98.00%
- CAS No.: 2996101-49-4
- Molecular Weight:145.66 kDa
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Storage:Shipping with dry ice
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Isotype
Human IgG4 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
TMPRSS6
In Vitro
Exerenibart (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].
Exerenibart 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.
In Vivo
Exerenibart (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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
Format
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Human IgG4 kappa
Application
ELISA, FACS, Functional assay
Chemical Information
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CAS No. 2996101-49-4
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Appearance Liquid
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Molecular Weight 145.66 kDa
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Color Colorless to light yellow
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SMILES
N/A
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Synonyms
REGN7999
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Exerenibart Related Classifications
HY-P991637 Related Classifications
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