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SB225002

SB225002 是一种有效的选择性 CXCR2 非肽拮抗剂，抑制 125I-IL-8 和 CXCR2 结合的 IC50 为 22 nM。

货号：
TK0592
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	182498-32-4
生物活性	SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits I-IL-8 binding to CXCR2 with an IC50 of 22 nM.
分子式	C13H10BrN3O4
分子量	352.14
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, stored under nitrogen
溶解性数据	DMSO : ≥ 100 mg/mL (283.98 mM)
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.
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%.
文献	•Nat Commun. 2020 Feb 28;11(1):1126. •Bioact Mater. 6 (2021) 2039-2057. •Cancer Res. 2018 Oct 1;78(19):5586-5599. •J Autoimmun. 2018 May;89:30-40. •Int J Biol Sci. 2022; 18(3):1271-1287. •J Cell Physiol. 2021 Apr;236(4):3114-3128. •Neuropharmacology. 2018 Jun;135:34-47. •Mol Immunol. 2018 Aug 7;101:440-449. •Cytokine. 2022 Jan 5;151:155789. •Mol Med Rep. 2019 Aug;20(2):1065-1074. •Exp Biol Med. 2020 Mar;245(6):562-575. •Research Square Preprint. 2022 Jan. •Molecular Biomedicine. 05 December 2021 •Research Square Preprint. 2021 Aug. •Research Square Preprint. 2020 Oct.
纯度及产品资料	98%

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