Home Immunology & Inflammation Complement System inhibitor Compstatin

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Compstatin Complement System inhibitor

Cat.No.S8522

Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
Compstatin Complement System inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 1550.77

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Quality Control

Batch: S852201 Water]100 mg/mL]false]]]false]]]false Purity: 99.85%
99.85

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPE cells Function assay 50 uM Inhibition of complement activation in human fetal RPE cells assessed as reduction in C5b-9 formation at 50 uM by fluorescence assay in presence of complement-competant human serum 25494040
fetal RPE cells Function assay 15 mins Inhibition of complement activation in human fetal RPE cells assessed as hemolysis of serum-treated rabbit erythrocytes compound preincubated with serum for 15 mins measured 20 mins after erythrocyte addition by hemolytic assay 25494040
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Solubility

In vitro
Batch:

Water : 100 mg/mL

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 1550.77 Formula

C66H99N23O17S2

 Storage (From the date of receipt)
CAS No. 206645-99-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCC(C)C(C(=O)NC1CSSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)C(C)C)C(C)C)CCC(=O)N)CC(=O)O)CC2=CNC3=CC=CC=C32)CC4=CN=CN4)CC5=CN=CN5)CCCN=C(N)N)C(=O)NC(C(C)O)C(=O)N)N

Mechanism of Action

Targets/IC50/Ki
complement component C3
12 μM
In vitro

Compstatin binds to native C3 and inhibits its cleavage by C3 convertase. Binding of this compound to native C3 is a multistep reaction that is preferred over its binding to the C3 fragments C3b and C3c. N-acetylation of this compound provides stability against enzymatic degradation.

This compound features a high selectivity for human and primate C3. While binding to C3 from baboons and other primates shows comparable interaction profiles as its human counterpart, no binding is detected for C3 from lower mammalian species such as mice, rats, guinea pigs, rabbits, or pigs.
In vivo

Compstatin completely inhibits in vivo heparin-induced complement activation without adverse effects on heart rate or systemic arterial, central venous, and pulmonary arterial pressures. This compound is a safe and effective complement inhibitor that has the potential to prevent complement activation during and after clinical cardiac surgery. Furthermore, it can serve as the prototype for designing an orally administrated drug. In the extracorporeal circulation model, this peptide inhibits the generation of C3a and C5a, the formation of the membrane attack complex, and CD11b expression on neutrophils (PMNs). The peptide also inhibits binding of C3/C3 fragments, PMNs, and monocytes to the polymer surface.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17684013/
  • [5] https://pubmed.ncbi.nlm.nih.gov/34388364/

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