SB225002, a potent, selective and non-peptideCXCR2antagonist, inhibits¹²⁵I-IL-8 binding toCXCR2with anIC₅₀of 22 nM.

SB225002 (SB 225002) is an antagonist of¹²⁵I-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 (IC₅₀values 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 IC₅₀values 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 IC₅₀values 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%^[2].

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^[4].

352.14

Solid

C₁₃H₁₀BrN₃O₄

182498-32-4

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

DMSO : ≥ 100 mg/mL(283.98 mM)

*"≥" means soluble, but saturation unknown.

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℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (7.10 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• 2.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.08 mg/mL (5.91 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.91 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 2.08 mg/mL (5.91 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (5.91 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明