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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。 |
描述 | The CXC chemokine receptor 2 (CXCR2) mediates chemotaxis of leukocytes and controls the extravasation and activation of neutrophils. Danirixin is a small-molecule, selective, and reversible CXCR2 antagonist[2]. Danirixin competes with CXCL8 binding to the membranes prepared from Chinese hamster ovary cells transfected with human CXCR2 or CXCR1 with IC50 values of 12.5nM (pIC50 = 7.90 ± 0.04) and 977nM (pIC50 = 6.03 ± 0.05), respectively. It also acts as a competitive antagonist against CXCL8 in Ca2+ mobilization assays with a Kb of 6.5nM and a pA2 of 8.44. Oral administration of Lewis rats with danirixin at doses of 0.3, 3, and 30mg/kg increased the EC50 value for CXCL2-induced CD11b expression in neutrophils from 4.5nM (the vehicle-treated group) to 9.4, 11.9, and 38.1nM, respectively. In fasted rats following inhaled lipopolysaccharide challenge, danirixin at a dosage of 10 mg/kg led to 84% inhibition of neutrophil influx to the lung with an ED50 value of 1.4mg/kg. In fed rats, 10mg/kg of danirixin resulted in 64% inhibition with an ED50 value of 2.3 mg/kg. Danirixin also dose-dependently inhibited neutrophils when administered to fasted rats 1 hour prior to ozone exposure with an ED50 value of 16.0 mg/kg[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.31mL 2.26mL 1.13mL |
22.63mL 4.53mL 2.26mL |
CAS号 | 954126-98-8 |
分子式 | C19H21ClFN3O4S |
分子量 | 441.904 |
别名 | GSK1325756 |
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 |
溶解度 |
DMSO: 6 mg/mL(13.58 mM),配合低频超声,并水浴加热至45℃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 |
动物实验配方 |