| 产品描述: | BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease |
| 靶点: |
IC50: 96 nM (mouse 11β-HSD1) IC50: 3341 nM (human 11β-HSD1);Dehydrogenase |
| 体外研究: |
BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 µM) reduces MCP-1 expression in fully differentiation adipocytes. BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium in J774.1 macrophages by Elisa. RT-PCR Cell Line: Differentiation adipocytes Concentration: 100 μM Incubation Time: 24 hours Result: Down-regulated MCP-1 mRNA level. |
| 体内研究: |
BVT-2733 (oral administration; 100 mg/kg; twice daily; 2 weeks) attenuates the arthritis severity and anti-CII level and decreases the levels of serum TNF-α, IL-1β, IL-6 and IL-17 in CIA mice. BVT 2733 (oral administration; 100 mg/kg; dosed (09.00 and 17.00 h); last 4 weeks) exhibits decreased body weight and enhanced glucose tolerance and insulin sensitivity when it compares to control mice. It also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo. Animal Model: Collagen-induced arthritis (CIA) mice Dosage: 100 mg/kg Administration: Oral administration; twice daily; 2 weeks Result: Reduced synovial inflammation and joint destruction. Animal Model: C57BL/6J mice Dosage: 100 mg/kg Administration: Oral administration; dosed (09.00 and 17.00 h); last 4 weeks Result: Improved metabolic homeostasis and suppressed the inflammation of adipose tissue in diet-induced obese mice. |
| 参考文献: |
1. 11β-hydroxydehydrogenase 1 (11β-HSD1) Inhibitor in Development 2. Zhang L, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94. 3. Wang L, et al. BVT.2733, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, attenuates obesity and inflammation in diet-induced obese mice. PLoS One. 2012;7(7):e40056. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.331 ml |
11.656 ml |
23.312 ml |
| 5 mM |
0.466 ml |
2.331 ml |
4.662 ml |
| 10 mM |
0.233 ml |
1.166 ml |
2.331 ml |
| 50 mM |
0.047 ml |
0.233 ml |
0.466 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。 |