SB-265610是一种有效的CXCR2拮抗剂,抑制CINC-1介导的Ca²⁺动员(IC50值为3.4 nM),而不抑制C5a介导的Ca²⁺动员(IC50值为6800 nM),并抑制CINC诱导的趋化作用,减轻体内炎性肺损伤中的中性粒细胞积聚。
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产品名称 | CXCR1 ↓ ↑ | CXCR2 ↓ ↑ | CXCR4 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Reparixin | ✔ | 99%+ | |||||||||||||||||
SB225002 |
+++
CXCR2, IC50: 22 nM |
99%+ | |||||||||||||||||
Plerixafor |
++
CXCR4, IC50: 44 nM |
99% | |||||||||||||||||
AMD 3465 6HBr | ✔ | 98% | |||||||||||||||||
WZ811 |
++++
CXCR4, EC50: 0.3 nM |
99% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
Concentration | Treated Time | Description | References | |
CHO cells expressing human CXCR2 receptor | 1-30 nM | 2 hours | To investigate the effect of SB265610 on [125I]-IL-8 binding, results showed that SB265610 reduced the maximal binding of [125I]-IL-8 without affecting the Kd. | Br J Pharmacol. 2009 Sep;158(1):328-38 |
Human neutrophils | 10-1000 nM | 30 minutes | To investigate the effect of SB265610 on GROα-stimulated chemotaxis, results showed that SB265610 caused a rightward shift of the concentration-response curves to GROα, but no effect on the maximal response. | Br J Pharmacol. 2009 Sep;158(1):328-38 |
Administration | Dosage | Frequency | Description | References | ||
Sprague-Dawley rats | Bronchopulmonary dysplasia (BPD) model | Intraperitoneal injection | 1 mg/kg | Administered on P1, P3, and P5 | CXCR2 antagonist significantly attenuated the LPS-induced increase in neutrophil counts in BALF and PB and restored alveolarization, as indicated by decreased mean cord length and increased alveolar surface area. | Clin Exp Pediatr. 2021 Jan;64(1):37-43 |
C57 black mice | CXCR2 wild type mice | Oral | 100 mg/kg/day | Once daily for 5 days | To evaluate the effect of CXCR2 antagonist on wound healing. Results showed that SB-265610 markedly delayed the wound healing process and reduced MPO activity at the wound site. | Wound Repair Regen. 2003 May-Jun;11(3):213-9 |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.80mL 0.56mL 0.28mL |
14.00mL 2.80mL 1.40mL |
28.00mL 5.60mL 2.80mL |
CAS号 | 211096-49-0 |
分子式 | C14H9BrN6O |
分子量 | 357.16 |
SMILES Code | O=C(NC1=C2NN=NC2=C(C#N)C=C1)NC3=CC=CC=C3Br |
MDL No. | MFCD09971124 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
DMSO: 50 mg/mL(139.99 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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
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