1140525-25-2

Usage

Uses

Used in Pharmaceutical Industry:
SB 290157 trifluoroacetate salt is used as an anti-inflammatory agent for its ability to selectively block the anaphylatoxin C3a receptor. This action helps in reducing inflammation and modulating the immune response, making it a promising candidate for the development of new therapeutic strategies to treat various inflammatory conditions.
Used in Research Applications:
In the field of scientific research, SB 290157 trifluoroacetate salt is used as a valuable tool to study the role of C3aR in various biological processes. By blocking the receptor, researchers can gain insights into the underlying mechanisms of inflammation and immune response, which can contribute to the development of novel therapeutic approaches.
Used in Drug Development:
SB 290157 trifluoroacetate salt is utilized in the development of new drugs targeting the anaphylatoxin C3a receptor. Its high affinity and selectivity make it an ideal starting point for designing and optimizing new molecules with improved pharmacological properties, potentially leading to more effective treatments for inflammatory diseases.
Used in Diagnostic Applications:
The compound can also be employed in diagnostic applications to identify and assess the presence of C3aR in various samples, such as blood or tissue samples. This can help in the early detection and monitoring of inflammatory conditions, as well as in the evaluation of the effectiveness of treatments targeting the C3aR pathway.

Biological Activity

sb 290157 is a c3ar antagonist.the anaphylatoxin c3a, a potent chemotactic peptide and inflammatory mediator, binds to and activates a g-protein-coupled receptor. molecular cloning of the c3ar has facilitated the identification of the non-peptide c3ar antagonists.

Biochem/physiol Actions

Target IC50: 200 nM against the anaphylatoxin C3a receptor; 7, 12.5, and 27.7 nM, in blocking C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR

in vitro

sb 290157 was a competitive antagonist of 125i-c3a and binding to rat basophilic leukemia (rbl)-2h3 cells expressing the human c3ar , with an ic50 of 200 nm. sb 290157 could also block the c3a-induced c3ar internalization concentration-dependently and c3a-induced ca21 mobilization in rbl-c3ar cells and human neutrophils. sb 290157 was founf to be selective for the c3ar in that it did not antagonize the c5ar or six other chemotactic g protein-coupled receptors. in addition, sb 290157 could also inhibit c3a induced ca21 mobilization of rbl-2h3 cells expressing the mouse and guinea pig c3ars [1].

in vivo

in animal models, sb 290157 was able to inhibit neutrophil recruitment in a guinea pig lps-induced airway neutrophilia model and decrease paw edema in a rat adjuvant-induced arthritis model [1].

IC 50

200 nm

references

[1] r. s. ames, d. lee, j. j. foley, et al. identification of a selective nonpeptide antagonist of the anaphylatoxin c3a receptor that demonstrates antiinflammatory activity in animal models. journal of immunology 166(10), 6341-6348 (2001).