SB-747651A diHydrochloride

SB-747651A diHydrochlorideCAS号: 1781882-72-1分子式: C16H24Cl2N8O分子量: 415.32描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC 50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride has potential for inflammation research [1].
纯度
97%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:50 mg/mL (120.39 mM)
生物活性
In vitro(体外研究)
SB-747651A dihydrochloride (5 μM; neutrophils) affects CXCL2-induced intraluminal crawling of neutrophils in a Mac-1-dependent manner. SB-747651A dihydrochloride prevents the intraluminal crawling of adherent neutrophils to optimal sites of emigration. SB-747651A dihydrochloride (5 μM; neutrophils) significantly increases transmigration time and detachment time. SB-747651A dihydrochloride affects mechanisms that regulate transendothelial migration of neutrophils in response to CXCL2 chemotactic gradient. SB-747651A dihydrochloride inhibits the migration speed of extravascular chemotaxing neutrophils but does not affect their directionality in response to CXCL2 chemotactic gradient [2].
In vivo(体内研究)
SB747651A (3 mg/kg; intrascrotal injection) dihydrochloride causes increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2 [3]. SB-747651A (3 mg/kg; i.p.) dihydrochloride affects neutrophil extravasation by increasing neutrophil emigration only at 3 and 4 hours in mouse peritonitis model of acute inflammation [3]. Animal Model: Male C57BL/6N mice (8~16 weeks) [3] Dosage: 3 mg/kg Administration: Intrascrotal injection Result: Resulted in increased neutrophil adhesion 3.5~4.5 hours following stimulation with CXCL2 as compared to the effect of CXCL2.