Ebribafusp alfa
Based on 1 Customer Validation
Ebribafusp alfa (ADX-097) comprising a humanized anti-C3d monoclonal antibody linked to two moieties of the first five consensus repeats of factor H (fH1-5). Ebribafusp alfa binds C3d and related fragments, catalyzes AP convertase dissociation, acts as a factor I co-factor for C3b cleavage, and delivers fH1-5 moieties to C3d-deposited tissues for local complement inhibition without systemic blockade. Ebribafusp alfa reduces glomerular C3 deposition, proteinuria, urine albumin-creatinine ratios, and urine soluble C5b-9 levels, preserves podocyte foot-process architecture, inhibits skin complement activation, and localizes to UVB-damaged primate skin. Ebribafusp alfa can be used for the research of membranous nephropathy, bullous pemphigoid, discoid lupus erythematosus, C3 glomerulopathy, IgA nephropathy, and lupus nephritis.
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- Pureza: 96.40%
- No. CAS: 2839652-75-2
- Peso molecular:213.781 kDa
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Human IgG4 kappa
Human
Complement C3d
Ebribafusp alfa (10-4,200 RU; 120 s injection, 180 s dissociation) binds recombinant human C3d with avidity-dependent affinity, showing a >2,000-fold increase in binding strength as C3d surface density increases 420-fold from 10 RU to 4,200 RU[2].
Ebribafusp alfa (IC50 concentrations) selectively inhibits the human alternative complement pathway with high potency (IC50 = 81 nM) and exhibits ~7.5-fold weaker activity against the classical complement pathway[2].
Ebribafusp alfa (IC50 concentrations) inhibits complement activity in human, mouse, and rat serum, with highest potency in rat serum (IC50 = 99 nM) and similar potency in human and mouse serum[2].
Ebribafusp alfa retains factor I co-factor activity for fluid-phase C3b cleavage, with efficiency comparable to isolated fH1-5[2].
Ebribafusp alfa (0.056-7 μM) potently inhibits complement deposition on human skin explants exposed to bullous pemphigoid serum, with significant inhibition observed at concentrations ≥0.28 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ebribafusp alfa (5 mg/kg; i.v.; single dose) durably inhibits glomerular complement deposition in CfH-/- mice by localizing to complement-active glomeruli[2].
Ebribafusp alfa (1-30 mg/kg; i.v.; single dose; 0.3-3 mg/kg; s.c.; single dose) reduces proteinuria and glomerular complement deposition in rat passive Heymann nephritis, with doses ≤10 mg/kg i.v. or ≤3 mg/kg s.c. showing no systemic complement inhibition[2].
Ebribafusp alfa (1-30 mg/kg; s.c.; single dose) localizes to complement-active primate skin at doses as low as 1 mg/kg s.c., with transient systemic complement inhibition only observed at higher doses[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:strain not specified[1]
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Dosage:1 mg/kg (s.c.); 1 mg/kg (i.v.)
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Administration:s.c.; single dose; i.v.; single dose
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Result:Inhibited glomerular complement activation.
Significantly reduced urine protein-creatinine and albumin-creatinine ratios.
Demonstrated efficacy equivalent to daily systemic complement blockade with cobra venom factor.
Left systemic complement activity (measured via serum zymosan assays) uninhibited.
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Animal Model:C57BL/6 CfH-/- (factor H-deficient)[2]
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Dosage:5 mg/kg
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Administration:i.v.; single dose
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Result:Significantly and durably reduced glomerular C3 fragment deposition.
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Animal Model:Cynomolgus monkeys (2-5 years of age)[2]
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Dosage:1 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:s.c.; single dose
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Result:Localized to UVB-exposed skin, with total tissue drug exposure dose-correlated and significantly greater than PBS control (p < 0.02).
Showed no systemic complement inhibition at 1 mg/kg dose.
Caused transient systemic complement inhibition at 10 mg/kg and 30 mg/kg doses that waned as circulating drug levels dropped below ~70 μg/mL.
Showed a trend toward reduced tissue complement inhibition at all tested doses, reaching maximal inhibition roughly 3 days after dosing.
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Animal Model:Sprague-Dawley (male, 6 weeks old, passive Heymann nephritis induced by two i.v. doses of anti-Fx1A antibody at 100 mg/kg on day 0 and 300 mg/kg on day 1)[2]
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Dosage:1-30 mg/kg (i.v.); 0.3-3 mg/kg (s.c.)
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Administration:i.v.; single dose; s.c.; single dose
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Result:Reduced glomerular C3 fragment deposition by ~40% at 1 mg/kg i.v. (p < 0.002).
Reduced glomerular C3 fragment deposition by ~75% at 3 mg/kg i.v. (p < 0.0001).
Reduced glomerular C3 fragment deposition to non-diseased control levels at ≥10 mg/kg i.v.
Did not affect systemic complement activity at doses ≤10 mg/kg i.v., while 30 mg/kg i.v. inhibited serum complement.
Reduced uPCR progression at all i.v. doses (p < 0.0001) with no dose-response observed.
Significantly reduced glomerular C3 fragment deposition at 1 mg/kg s.c. (p < 0.05) and 3 mg/kg s.c. (p < 0.0001 vs. anti-Fx1A + PBS).
Showed dose-dependent reduction in uPCR at all s.c. doses by day 7 (p < 0.005).
Reduced uPCR AUC by 73% at 3 mg/kg s.c. (p < 0.003).
Reduced uPCR AUC by 59% at 1 mg/kg s.c. (p < 0.01).
Reduced urine C5b-9/creatinine ratio AUC at 1 mg/kg s.c. (p < 0.03) and 3 mg/kg s.c. (p < 0.002 vs. untreated anti-Fx1A).
Rescued podocyte architecture, reducing foot-process effacement compared to untreated PHN rats at 3 mg/kg s.c.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Human IgG4 kappa
ELISA, FACS, Functional assay
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Immobilized CD3D-CD3E Heterodimer Protein, Human (HEK293, HY-P72726) can bind Ebribafusp alfa. The ED50 for this effect is 100.4 ng/mL.
Chemical Information
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No. CAS 2839652-75-2
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Appearance Liquid
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Peso molecular 213.781 kDa
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Color Colorless to light yellow
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SMILES
[Ebribafusp alfa]
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Synonyms
ADX-097
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Envío
Shipping with dry ice.
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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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Ficha de datos (266 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)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ebribafusp alfa Related Classifications
HY-P990955 Related Classifications
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