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Description

A non-peptide with anti-inflammatory properties that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (C3aR, IC50 = 200 nM). Does not antagonize C5aR or other chemotactic G-protein coupled receptors. Blocks 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 (IC50 = 7, 12.5, and 27.7 nM, respectively). Also blocks C3a-mediated ATP release from guinea pig platelets (IC50 = 30 nM)., A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC50 = 200 nM). Does not antagonize C5aR or other chemotactic G-protein-coupled receptors. Blocks 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 (IC50 = 7, 12.5, and 27.7 nM, respectively). Also blocks C3a-mediated ATP release from Guinea pig platelets (IC50 = 30 nM). Exhibits anti-inflammatory properties. Supplied as a trifluoroacetate salt.