Compstatin

Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.

Compstatin Chemical Structure

Compstatin Chemical Structure

CAS No. 206645-99-0

Purity & Quality Control

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

Compstatin Related Products

Cell Data

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
Click to View More Cell Line Experimental Data

Biological Activity

Description Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
Targets
complement component C3 [4]
12 μM
In vitro
In vitro

Compstatin binds to native C3 and inhibits its cleavage by C3 convertase. Binding of Compstatin to native C3 is a multistep reaction that is preferred over its binding to the C3 fragments C3b and C3c. N-acetylation of Compstatin provides stability against enzymatic degradation[1].

Compstatin 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[3].

Cell Research Cell lines iPSC-ECs
Concentrations 50 μM
Incubation Time 2 days
Method

Cells were treated with indicated concentration of drug for 2 days.

In Vivo
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. Compstatin is a safe and effective complement inhibitor that has the potential to prevent complement activation during and after clinical cardiac surgery. Furthermore, Compstatin can serve as the prototype for designing an orally administrated drug. In the extracorporeal circulation model, Compstatin 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[2].

Animal Research Animal Models Juvenile baboons (P. anubis)
Dosages 17, 21, 34, 38.5, 50, 63.5 mg/kg
Administration by bolus injection, infusion, or both

Chemical Information & Solubility

Molecular Weight 1550.77 Formula

C66H99N23O17S2

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

In vitro
Batch:

Water : 100 mg/mL


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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