| Bioactivity | Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1]. | ||||||
| Target | Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)EC50: 5.8 nM (hMC1R), 5.3nM (hMC3R), 0.27 nM (hMC4R), 0.28 (rMC4R), 1600 nM (hMC5R) | ||||||
| Invitro | 黑皮质素受体激动剂在大脑中起作用以调节食物摄入和体重，并且独立于这些作用。Setmelanotide 对人和大鼠 MC4R 具有激动剂活性，Ki 分别为 2.1 和 2.7 nM，EC50 分别为 0.27 和 0.28 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Setmelanotide 相关抗体: | ||||||
| In Vivo | Setmelanotide 对禁食过夜后的再进食的抑制取决于功能性 MC4R，不需要 MC3R。BIM-22493 可显著改善葡萄糖稳态。与对照组相比，用 BIM-22493 处理的 Lepob/Lepob 小鼠表现出显著改善的葡萄糖清除率。慢性 BIM-22493 处理与显著降低的血糖水平和 HOMA-IR 值相关[1]。在饮食诱导的肥胖非人灵长类动物模型中，经过 8 周的处理 (13.5%)，使用 Setmelanotide 处理会导致食物摄入量暂时减少 (35%)，体重持续下降[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||
| CAS | 920014-72-8 | ||||||
| Formula | C49H68N18O9S2 | ||||||
| Molar Mass | 1117.31 | ||||||
| Appearance | 固体 | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage | Sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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| Reference | [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 resistance, and improves cardiovascular function in diet-induced obese rhesus macaques. Diabetes. 2013 Feb;62(2):490-7. |
Setmelanotide
CAS: 920014-72-8 F: C49H68N18O9S2 W: 1117.31
Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human
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