产品描述: | Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively |
靶点: |
pKi: 8.1 (p38α), 7.6 (p38β);p38MAPK; Autophagy |
体内研究: |
In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β) |
参考文献: |
1. Willette RN, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70. 2. Zhang XM, et al. Suppression of mitochondrial fission in experimental cerebral ischemia: The potential neuroprotective target of p38 MAPK inhibition. Neurochem Int. 2015 Nov;90:1-8. |
溶解性: |
Ethanol : 33.33 mg/mL (86.92 mM; Need ultrasonic) DMSO : 27.5 mg/mL (71.72 mM; Need ultrasonic) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.608 ml |
13.039 ml |
26.078 ml |
5 mM |
0.522 ml |
2.608 ml |
5.216 ml |
10 mM |
0.261 ml |
1.304 ml |
2.608 ml |
50 mM |
0.052 ml |
0.261 ml |
0.522 ml |
|
注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |