SB 290157 trifluoroacetate

Biological Activity

SB 290157 trifluoroacetate is a potent C3a receptor antagonist (IC₅₀ values are 27 - 30 nM for C3a-induced Ca²⁺ mobilization in vitro and ex vivo). Inhibits C3a-induced chemotaxis in human mast cell line. Also inhibits tau hyperphosphorylation in vitro. Displays anti-inflammatory effects in animal models of airway inflammation and arthritis. Also inhibits glucose-induced insulin secretion and ATP production from ex vivo human and mouse pancreatic islets. Also exhibits C3a receptor agonist activity.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models.
   Ames et al.
   J.Immunol., 2001;166:6341
2. C3aR and C5aR1 act as key regulators of human and mouse β-cell function.
   Atanes et al.
   Cell Mol.Life Sci., 2018;75:715
3. Complement C3a receptor antagonist attenuates tau hyperphosphorylation via glycogen synthase kinase 3β signaling pathways.
   Hu et al.
   Eur.J.Pharmacol., 2019;850:135
4. The C3a receptor antagonist SB 290157 has agonist activity.
   Mathieu et al.
   Immunol.Lett., 2005;100:139

Product Datasheets