SB290157 (SB 290157) is a potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.
SB290157 does not antagonize the C5aR or 5 other chemotactic GPCRs on human neutrophils.
SB290157 blocks C3a-induced C3aR internalization and C3a-induced Ca(2+) mobilization in RBL-C3aR cells and human neutrophils with IC50 of 27.7 and 28 nM, respectively.
SB290157 also inhibits C3a-induced Ca2+ mobilization of mouse and guinea pig C3aRS with IC50 of 7 and 12.5 nM, respectively.
SB290157 potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the contractile response to field stimulation of perfused rat caudal artery, demonstrates antiinflammatory activity in animal models.
Physicochemical Properties
M.Wt
412.49
Formula
C22H28N4O4
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
N(2)-[(2,2-diphenylethoxy)acetyl]-L-arginine
References
1. Ames RS, et al. J Immunol. 2001 May 15;166(10):6341-8.
