货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V53215-1ml	10mM in DMSO	￥4560.00 V53215-1ml ￥4560.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V53215-1ml

10mM in DMSO

￥4560.00

货期：3-5天

产品名称:

setmelanotide

规格或纯度:

Moligand™

作用类型:

激动剂

作用机制:

黑色素皮质受体 4 激动剂

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

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

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。

参考文献

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