Compstatin

Catalog No.S8522 Batch:S852201

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Technical Data

Formula

C66H99N23O17S2

Molecular Weight 1550.77 CAS No. 206645-99-0
Solubility (25°C)* In vitro Water 100 mg/mL (64.48 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].

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].

Protocol (from reference)

Cell Assay:

[5]

  • Cell lines

    iPSC-ECs

  • Concentrations

    50 μM

  • Incubation Time

    2 days

  • Method

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

Animal Study:

[2]

  • Animal Models

    Juvenile baboons (P. anubis)

  • Dosages

    17, 21, 34, 38.5, 50, 63.5 mg/kg

  • Administration

    by bolus injection, infusion, or both

Selleck's Compstatin has been cited by 3 publications

Peptidoglycan from Bacillus anthracis Inhibits Human Macrophage Efferocytosis in Part by Reducing Cell Surface Expression of MERTK and TIM-3 [ bioRxiv, 2023, 2023.03.30.535001] PubMed: 37066181
Low molecular weight polysialic acid binds to properdin and reduces the activity of the alternative complement pathway [ Sci Rep, 2022, 12(1):5818] PubMed: 35388026
Patient-specific iPSC-derived endothelial cells reveal aberrant p38 MAPK signaling in atypical hemolytic uremic syndrome [ Stem Cell Reports, 2021, 16(9):2305-2319] PubMed: 34388364

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.