VX-702CAS号: 745833-23-2;479543-46-9分子式: C19H12F4N4O2分子量: 404.3描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
产品描述 | |
描述 |
VX-702是一种高选择性p38α MAPK抑制剂,作用于p38α比作用于p38β效果高14倍。 |
纯度 |
>98%
|
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 | |
别名 |
VX702; VX 702
|
可溶性/溶解性 |
DMSO : 81 mg/mL (200.34 mM)
|
生物活性 | |
靶点 |
p38α
|
In vitro(体外研究) |
Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or JPence of anti-platelet therapies. VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner.
|
In vivo(体内研究) |
The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally. VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.
|
参考文献 | |
参考文献 |
[1] Kuliopulos A, et al. Thromb Haemost, 2004, 92(6), 1387-1393. |
分子结构图