SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
IC50&Target
I-IL-8-CXCR2
22 nM (IC50, in CHO cell membrane)
体外研究
SB225002 (SB 225002) is an antagonist of I-IL-8 binding to CXCR2 with an IC50=22 nM. SB225002 shows >150-fold selectivity over CXCR1 and four other 7-TMRs tested. SB225002 is a potent antagonist of rabbit CXCR2, inhibiting rabbit PMN chemotaxis in response to optimal concentrations of human IL-8 or GROα (IC50 values of 30 and 70 nM, respectively. In these cells (PMN, HL60, CXCR1-RBL-2H3), SB225002 produces a concentration-dependent inhibition of both IL-8- and GROα-mediated calcium mobilization with IC50 values of 8 and 10 nM, respectively. In 3ASubE cells stably transfected with CXCR2, SB 225002 dose-dependently inhibits calcium mobilization induced by both GROα and IL-8, with IC50 values of 20 and 40 nM, respectively. WHCO1 cells treated with SB225002 exhibits a 40% reduction in cell proliferation. Blocking CXCR2 signaling in WHCO1 cells with 400 nM SB225002 (SB 225002) significantly decreases cell proliferation by ~40% to 50%.
体内研究
SB225002 (SB 225002) selectively blocks IL-8-induced neutrophil margination in rabbits. CXCR2 is blocked using the selective antagonist SB225002 (2 mg/kg) or neutralizing CXCR2 antiserum. The CXCR2 antagonist SB225002 decreases neutrophil counts in ischemic hemispheres of ApoE mice on Western diet and wildtype mice on normal diet. SB225002 significantly attenuates microglial activation and BBB damage, increases myelination, and reduces astrogliosis in the white matter after LPS-sensitized HI.
分子式
C13H10BrN3O4
分子量
352.14
CAS号
182498-32-4
运输条件
Room temperature in continental US; may vary elsewhere.