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• 产品描述： Setmelanotide (RM-493, BIM-22493, CAM 4072) 是一种黑色皮质素-4 受体（melanocortin-4 receptor, MC4R）的环肽全激动剂，EC50 为 0.27 nM，Ki 为 2.1 nM

• 靶点： MC4R:0.27 nM(EC50); MC4:2.1 nM(Ki);MelanocortinReceptor

• 体外研究：
  Setmelanotide decreases TNF-α/IFN-γ-induced chemokine expression in astrocytes and increases IL-6 and IL-11 mRNA and protein secretion via MC4R. Setmelanotide Induces CREB phosphorylation in astrocytes and setmelanotide treated astrocytes secrete factors that are able to modulate macrophage polarization into an anti-inflammatory phenotype

• 体内研究：
  RM-493 and liraglutide co-treatment enhances weight loss in DIO mice and hypothalamic Glp-1r expression is higher in mice treated with the combination therapy after both acute and chronic treatment. Adjunctive administration of RM-493 and liraglutide improves glucose tolerance and insulin sensitivity, lowers fasting levels of glucose and insulin and decreases cholesterol levels beyond what can be achieved with the corresponding mono-therapies

• 细胞实验： Cell lines: U373 astrocytoma cells Concentrations: 0.001 μM –10 μM Incubation Time: 1h, 4 h Method: Cells were treated with 0.001–10 μM setmelanotide for 1 h and thereafter with TNF-α and IFN-γ for 4 h. For blocking experiments, 10 μM SHU9119 (26) was added 30 min before addition of setmelanotide during 4 h. Astrocytes stimulate with setmelanotide and or SHU9119 (10 μM) for 4 h, replace the medium with macrophage culture medium and add the medium to the macrophages 24 h thereafter. From the medium, 100 μL is collected in Eppendorf tubes and stored at −80°C for ELISA assays.

• 动物实验： Animal Models: Diet-induced obese mice Dosages: 3.6 μmol/kg/day Administration: s.c.

• 参考文献：
  1. Kong Y Chen, et al. RM-493, a melanocortin-4 receptor (MC4R) agonist, increases resting energy expenditure in obese individuals. J Clin Endocrinol Metab. 2015 Apr;100(4):1639-45. 2. Alwin Kamermans, et al. Setmelanotide, a Novel, Selective Melanocortin Receptor-4 Agonist Exerts Anti-inflammatory Actions in Astrocytes and Promotes an Anti-inflammatory Macrophage Phenotype. Front Immunol. 2019 Oct 4;10:2312. 3. Christoffer Clemmensen, et al. Dual melanocortin-4 receptor and GLP-1 receptor agonism amplifies metabolic benefits in diet-induced obese mice. EMBO Mol Med. 2015 Mar; 7(3): 288–298.

• 溶解性： Soluble  in  DMSO、H2O、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	0.895 ml	4.475 ml	8.95 ml
  5 mM	0.179 ml	0.895 ml	1.79 ml
  10 mM	0.09 ml	0.448 ml	0.895 ml
  50 mM	0.018 ml	0.09 ml	0.179 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *