| 产品描述: | A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases |
| 靶点: |
IC50: 20 nM (E-selectin), 25 nM (ICAM-1);Integrin |
| 体内研究: |
A-205804 (5 mg/kg; p.o.) shows a half-life of 1 hour for rat.A-205804 (10 mg/kg; p.o.; 3 times per week; for 2 weeks) attenuates the E-selectin expression on the endothelial vascular niche cells in mice. Animal Model: C57BL/6 mice Dosage: 10 mg/kg Administration: Oral administration, 3 times per week, for 2 weeks Result: Efficiently decreased the expression of E-selectin on the endothelial vascular niche cells Animal Model: Rat Dosage: 5 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: t1/2 = 1 hour |
| 参考文献: |
1. Stewart AO, et al. Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem. 2001 Mar 15;44(6):988-1002. 2. Morita K, et al. RUNX transcription factors potentially control E-selectin expression in the bone marrow vascular niche in mice. Blood Adv. 2018 Mar 13;2(5):509-515. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.329 ml |
16.645 ml |
33.289 ml |
| 5 mM |
0.666 ml |
3.329 ml |
6.658 ml |
| 10 mM |
0.333 ml |
1.664 ml |
3.329 ml |
| 50 mM |
0.067 ml |
0.333 ml |
0.666 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。 |