| Description | Setmelanotide (BIM-22493) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively). |
| In vitro | 黑色素皮质激素受体激动剂在大脑中作用为：调节食物摄入量和体重，影响胰岛素敏感性。Setmelanotide对人类及大鼠的MC4R展现出激动剂活性，其Kis分别为2.1 nM和2.7 nM，EC50s分别为0.27 nM和0.28 nM[1]。 |
| In vivo | BIM-22493在夜间禁食后重食的抑制依赖于功能性MC4R。BIM-22493能够急性改善葡萄糖稳态。在Lepob/Lepob小鼠中，BIM-22493表现出与对照组相比显著提高的葡萄糖清除率。长期治疗BIM-22493与血清胰岛素、葡萄糖和HOMA-IR值显著降低有关，表明胰岛素敏感性得到改善[1]。setmelanotide治疗会导致食物摄入量短暂下降(35%)，并在8周的治疗期间持续减重(13.5%)，这一结果在饮食诱导的肥胖非人灵长类模型中得到验证[2]。 |
| Target activity | MC4R (rat): 2.7 nM (ki), MC5R (human): 1600 nM (EC50), MC5R (human): 430 nM (ki), MC3R (human): 5.3nM (EC50), MC3R (human): 10 nM (ki), MC4R (rat):0.28 Nm (EC50), MC4R (human): 2.1 nM (ki), MC4R (human): 0.27 nM (EC50), MC1R (human):3.9 nM (ki), MC1R (human):5.8 nM (EC50) |
| Synonyms | BIM-22493, IRC-022493, RM-493 |
| molecular weight | 1117.31 |
| Molecular formula | C49H68N18O9S2 |
| CAS | 920014-72-8 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 100 mg/mL (89.50 mM), Sonication is recommended. DMSO: 100 mg/mL (89.50 mM), Sonication is recommended. |
| References | 1. Kumar KG, et al. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900. 2. Kievit P, et al. Chronic treatment with a melanocortin-4 receptor agonist causes weight loss, reduces insulin resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7. |