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Synonyms | BIM-22493, CAM 4072 | Storage (From the date of receipt) |
3 years -20°C powder | ||||||||
化学式 | C49H68N18O9S2
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分子量 | 1117.31 | CAS No. | 920014-72-8 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (89.5 mM) | ||||||||
Water | 100 mg/mL (89.5 mM) | ||||||||||
Ethanol | 100 mg/mL (89.5 mM) | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM. |
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in vitro | 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.[2] |
in vivo | 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.[3] |
細胞アッセイ | 細胞株 | U373 astrocytoma cells |
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濃度 | 0.001 μM –10 μM | |
反応時間 | 1h, 4 h | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Diet-induced obese mice |
投薬量 | 3.6 μmol/kg/day | |
投与方法 | s.c. |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。