Setmelanotide (RM-493)

製品コードE1002 バッチE100204

印刷

化学情報

Synonyms

BIM-22493, CAM 4072

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₄₉H₆₈N₁₈O₉S₂

分子量

1117.31

CAS No.

920014-72-8

Solubility (25°C)*

体外

DMSO

100 mg/mL (89.5 mM)

Ethanol

100 mg/mL (89.5 mM)

Water

50 mg/mL (44.75 mM)

体内（毎回新しく調製した物を用意してください）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5mg/ml (4.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.25mg/ml (0.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro	Setmelanotide (RM-493) decreases TNF-α/IFN-γ-induced chemokine expression in astrocytes and increases IL-6 and IL-11 mRNA and protein secretion via MC4R. It induces CREB phosphorylation in astrocytes, and this compound treated astrocytes secrete factors that are able to modulate macrophage polarization into an anti-inflammatory phenotype.^[2]
in vivo	Setmelanotide (RM-493) 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 this compound 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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U373 astrocytoma cells
	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 (RM-493) 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 this compound during 4 h. Astrocytes stimulate with it 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.
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.

参考

https://pubmed.ncbi.nlm.nih.gov/25675384/
https://pubmed.ncbi.nlm.nih.gov/31636637/
https://pubmed.ncbi.nlm.nih.gov/25652173/

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。