SB290157 trifluoroacetate

SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor (IC50 of 200 nM) . SB 290157 is a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR, IC50 of 200 nM) . SB 290157 blocks C3a-induced C3aR internalization in a concentration-dependent manner and C3a-induced Ca2+ mobilization in RBL-C3aR cells and human neutrophils (IC50s of 27.7 and 28 nM, respectively) . SB 290157 is selective for the C3aR in that. SB 290157 also inhibits C3a-induced Ca2+ mobilization of RBL-2H3 cells expressing the mouse and guinea pig C3aRs. It 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.Neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model inhibited by SB 290157 , SB 290157 decreases paw edema in a rat adjuvant-induced arthritis model[1]. The antagonist is able to reduce joint swelling only at 3 h, and about 50% inhibition of joint swelling is observed with the concentration of 30 mg/kg. The C3 level is significantly decreased at 3 h compared with naive mice showing complement consumption. Furthermore, the C3 activation is observed and increased corresponding to the graded concentration of anti-OVA pAb.

1140525-25-2

>98% (HPLC)

DMSO:125 mg/mL (237.41 mM; Need ultrasonic)

OC (=O) C (F) (F) F.NC (=N) NCCC[C@H] (NC (=O) COCC (c1ccccc1) c1ccccc1) C (O) =O

C24H29F3N4O6

526.51

Storage temperature: -20°C. Stability: ≥ 2 years