MSG606
Based on 1 Customer Validation
MSG606 is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 can delay pain hypersensitivity and reduce cholesterol levels. MSG606 can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.68%
- CAS 番号: 1416983-77-1
- 分子式: C62H82N20O13S
- 分子量:1347.51
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保管条件:
Sealed storage, away from moisture and light, under nitrogen.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
生物活性
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MC1R |
MSG606 (20 μM, 3 h) attenuates the NDP-MSH-stimulated increase in cAMP in T-47d and MCF7 cells[3].
MSG606 (20 μM, 6 h) inhibits cell proliferation in NDP-MSH-stimulated T-47d and MCF7 cells[3].
MSG606 (20 μM, 0-12 h) prolongs the time taken to transition from the G1 to the S phase in NDP-MSH-stimulated T-47d cells[3].
MSG606 (5-20 μM, overnight) decreases CREB, ATF-1, the phosphorylation of ERK and p-65 NFκB levels in NDP-MSH-stimulated T-47d, MCF7 and HEK 293 T cells[3].
MSG606 () inhibits the mRNA expression of IL-1β and TNFα in LPS ()-stimulated BMDMs[4].
MSG606 (1 μmol/L, 30 mins) attenuates the oxLDL-induced increase in LXRα expression in BMDMs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T-47d, MCF7 and HEK 293 T cells
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Concentration:5, 10 and 20 μM
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Incubation Time:Overnight
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Result:Decreased CREB, ATF-1, the phosphorylation of ERK and p-65 NFκB levels
MSG606 (7.5 μg, i.c.v) increases hyperalgesia latencies in Morphine-treated female mice[2].
MSG606 (1 mg/kg, i.p., daily for 4 weeks) reduces total cholesterol levels and increases markers of plaque stability in mice with cholesterol-rich high-fat diet[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Subarachnoid hemorrhage (SAH) rats models[1]
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Dosage:6 nM
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Administration:Intracerebrally injection, 1 h befor SAH
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Result:Increased levels of NFκB, IL-1β, and TNFα.
Reduced p-AMPK and p-TBK1.
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Animal Model:Mice with cholesterol-rich high-fat diet[4]
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Dosage:1 mg/kg
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Administration:Intraperitoneally injection, daily for 4 weeks
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Result:Reduced total cholesterol levels.
Increases markers of plaque stability.
increased hepatic ABCA1 and ABCG1 and LDL receptor mRNA levels.
Reduced monocyte counts in the aorta and modulates circulating monocyte profile.
化学情報
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CAS 番号 1416983-77-1
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性状 Solid
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分子量 1347.51
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分子式 C62H82N20O13S
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Color White to off-white
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シーケンスの短縮
{Bua}GH-{d-Phe}-R-{d-Trp}-CDRFG-NH2 (Carba sulfide bridge:Bua1-Cys7)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light, under nitrogen
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
溶剤 & 溶解度
H2O : ≥ 50 mg/mL (37.11 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Xu W, et al. Activation of Melanocortin 1 Receptor Attenuates Early Brain Injury in a Rat Model of Subarachnoid Hemorrhage viathe Suppression of Neuroinflammation through AMPK/TBK1/NF-κB Pathway in Rats. Neurotherapeutics. 2020;17(1):294-308 [Content Brief]
[2]. Juni A, et al. Sex-specific mediaion of opioid-induced hyperalgesia by the melanocortin-1 receptor. Anesthesiology. 2010 Jan;112(1):181-8. [Content Brief]
[3]. Chelakkot VS, et al. MC1R signaling through the cAMP-CREB/ATF-1 and ERK-NFκB pathways accelerates G1/S transition promoting breast cancer progression. NPJ Precis Oncol. 2023 Sep 7;7(1):85. [Content Brief]
[4]. Rinne P, et al. Melanocortin 1 Receptor Signaling Regulates Cholesterol Transport in Macrophages. Circulation. 2017 Jul 4;136(1):83-97. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.7421 mL | 3.7105 mL | 7.4211 mL | 18.5527 mL |
| 5 mM | 0.1484 mL | 0.7421 mL | 1.4842 mL | 3.7105 mL | |
| 10 mM | 0.0742 mL | 0.3711 mL | 0.7421 mL | 1.8553 mL | |
| 15 mM | 0.0495 mL | 0.2474 mL | 0.4947 mL | 1.2368 mL | |
| 20 mM | 0.0371 mL | 0.1855 mL | 0.3711 mL | 0.9276 mL | |
| 25 mM | 0.0297 mL | 0.1484 mL | 0.2968 mL | 0.7421 mL | |
| 30 mM | 0.0247 mL | 0.1237 mL | 0.2474 mL | 0.6184 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.