生物活性
SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
IC50 & Target[1]
125I-IL-8-CXCR2
22 nM (IC50, in CHO cell membrane)
体外研究
(In Vitro)
SB225002 (SB 225002) is an antagonist of 125I-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[1]. 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
(In Vivo)
SB225002 (SB 225002) selectively blocks IL-8-induced neutrophil margination in rabbits[1]. 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[3]. SB225002 significantly attenuates microglial activation and BBB damage, increases myelination, and reduces astrogliosis in the white matter after LPS-sensitized HI
分子量
352.14
性状
Solid
Formula
C13H10BrN3O4
CAS 号
182498-32-4
运输条件
Room temperature in continental US; may vary elsewhere.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.8398 mL 14.1989 mL 28.3978 mL
5 mM 0.5680 mL 2.8398 mL 5.6796 mL
10 mM 0.2840 mL 1.4199 mL 2.8398 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: