| 产品描述: | Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research. |
| 靶点: |
MC1R;MC3R |
| 体外研究: |
Resomelagon(0-10 mg/kg;腹腔注射、静脉注射、口服.;24 小时;雄性 C57BL/6J 野生型 (WT) 和 BALB/c 小鼠)促进体内急性炎症的消退[1 ]。 Resomelagon(25-50 mg/kg;口服;每日一次,持续 8 天;雄性 C57BL/6J 野生型 (WT) 和 BALB/c 小鼠)减少小鼠的关节炎[1]。 |
| 体内研究: |
Resomelagon(0-1000 μM;8 分钟;HEK293A 细胞)通过 ERK1/2 磷酸化和 Ca2+ 动员促进黑皮质素信号转导 。 Resomelagon(1 nM;30 分钟;腹膜巨噬细胞)具有抗炎活性并抑制 TNF-α 释放和胞吐作用。 |
| 参考文献: |
1. Montero-Melendez T, et, al. Biased agonism as a novel strategy to harness the proresolving properties of melanocortin receptors without eliciting melanogenic effects. J Immunol. 2015 Apr 1;194(7):3381-8. 2. WHO Drug Information. International Nonproprietary Names for Pharmaceutical |
| 保存条件: |
4°C, 避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.352 ml |
16.762 ml |
33.523 ml |
| 5 mM |
0.67 ml |
3.352 ml |
6.705 ml |
| 10 mM |
0.335 ml |
1.676 ml |
3.352 ml |
| 50 mM |
0.067 ml |
0.335 ml |
0.67 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。 |