1. Immunology/Inflammation
  2. Complement System
  3. SAR-443809

SAR-443809 is a selective alternative complement system inhibitor and monoclonal antibody targeting complement factor Bb. SAR-443809 blocks the cleavage of C3 and factor B by selectively binding to the activated form of factor Bb, with a KD of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for the research of hematological and renal disorders mediated by abnormal alternative complement pathway.

For research use only. We do not sell to patients.

SAR-443809

SAR-443809 Chemical Structure

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Description

SAR-443809 is a selective alternative complement system inhibitor and monoclonal antibody targeting complement factor Bb. SAR-443809 blocks the cleavage of C3 and factor B by selectively binding to the activated form of factor Bb, with a KD of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for the research of hematological and renal disorders mediated by abnormal alternative complement pathway[1].

Species Reactivity

Human

In Vitro

SAR-443809 (Human FB: 6-500 nM; human FBb: 0.4-30 nM; SAR443809 Fab: 3.7-300 nM; 25°C during assay) binds with high affinity to human factor Bb (KD = 7.3 nM) and cynomolgus factor Bb (KD = 61 nM), and its Fab fragment binds to the active alternative pathway C3 convertase (C3bBb) with high affinity (KD = 0.5 nM)[1].
SAR-443809 potently and selectively inhibits the human complement alternative pathway (IC50 = 8.47 μg/mL) and cynomolgus monkey complement alternative pathway (IC50 = 15.72 μg/mL) by blocking cleavage of C3 and factor B, without inhibiting the classical or lectin pathways[1].
SAR-443809 (50 minutes at 37°C) inhibits alternative pathway-mediated hemolysis of rabbit erythrocytes with an IC50 of 28.45 μg/mL[1].
SAR-443809 (50 minutes at 37°C) inhibits alternative pathway-mediated C3b deposition on rabbit erythrocytes with an apparent IC50 of 33.8 μg/mL[1].
SAR-443809 (100 μg/mL; 30 minutes at 37°C) inhibits unregulated fluid-phase C3 cleavage in factor H-depleted human serum, preventing consumption of C3 via alternative pathway tickover[1].
SAR-443809 selectively binds to human factor Bb (EC50 = 30.9 ng/mL) and shows no specific binding to other tested plasma serine proteases, including most complement system enzymes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SAR-443809 (15 mg/kg; i.v./s.c.; single dose) delivers sustained (≥ 288 hours) 90% inhibition of complement alternative pathway activity in female cynomolgus monkeys [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cynomolgus monkeys (female)[1]
Dosage: 15 mg/kg (i.v.); 15 mg/kg (s.c.)
Administration: i.v.; single dose
s.c.; single dose
Result: Achieved 90% inhibition of alternative pathway complement activity at 24 hours post-dose, sustained for at least 288 hours (i.v.).
Reached 90% inhibition of alternative pathway complement activity between 24-48 hours post-dose, sustained for at least 288 hours (s.c.).
Showed no classical pathway inhibition.
Gene ID

629  [NCBI]

Accession

AAH04143.1

Target

Complement Factor B/CFB

Application

ELISA, FACS, Functional assay

Conjugated

Unconjugated

Reconsititution

The product can be reconstituted/diluted with sterile PBS or saline.

Formulation

Please refer to the lot-specific COA for specific buffer information.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SAR-443809
Cat. No.:
HY-P992456
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