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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 96.40%
- CAS No.: 2839652-75-2
- Masse moléculaire:213.781 kDa
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
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.
-
Animal Model:strain not specified[1]
-
Dosage:1 mg/kg (s.c.); 1 mg/kg (i.v.)
-
Administration:s.c.; single dose; i.v.; single dose
-
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.
-
Animal Model:C57BL/6 CfH-/- (factor H-deficient)[2]
-
Dosage:5 mg/kg
-
Administration:i.v.; single dose
-
Result:Significantly and durably reduced glomerular C3 fragment deposition.
-
Animal Model:Cynomolgus monkeys (2-5 years of age)[2]
-
Dosage:1 mg/kg; 10 mg/kg; 30 mg/kg
-
Administration:s.c.; single dose
-
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.
-
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]
-
Dosage:1-30 mg/kg (i.v.); 0.3-3 mg/kg (s.c.)
-
Administration:i.v.; single dose; s.c.; single dose
-
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.
-
Human IgG4 kappa
ELISA, FACS, Functional assay
-
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
-
CAS No. 2839652-75-2
-
Appearance Liquid
-
Masse moléculaire 213.781 kDa
-
Color Colorless to light yellow
-
SMILES
[Ebribafusp alfa]
-
Synonyms
ADX-097
-
Livraison
Shipping with dry ice.
-
Formulation
Please refer to the lot-specific COA for specific buffer information.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
-
Fiche technique (266 KB)
-
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)
-
Inhibitory Antibodies User Guide (603 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ebribafusp alfa Related Classifications
HY-P990955 Related Classifications
Powered by Bioz