VX-702 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
説明
VX-
702 is a third generation inhibitor of p38 mitogen-
activated protein (MAP) kinases, binding to both p38α and p38β (K
d = 3.7 and 17 nM, respectively) in an ATP-
competitive fashion. It inhibits IL-
6, IL-
1β, and TNF-
α production in LPS-
primed blood with IC
50 values of 59, 122, and 99 ng/ml, respectively. VX-
702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-
46619 , or collagen but does not block platelet aggregation in response to collagen. Although orally active, VX-
702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.
使用
VX-702 is a p38 mitogen-activated protein kinase (MAPK) inhibitor. VX-702 had no effect on platelet aggregation induced by any of the p38 MAPK agonists. VX-702 has potential use in the treatment of inflammation, rheumatoid arthritis and cardiovascular diseases.
VX-702 上流と下流の製品情報
原材料
準備製品