MSG606 TFA
MSG606 TFA is a selective melanocortin 1 receptor (MC1R) antagonist. MSG606 TFA can abolish the neuroprotective effects of BMS-470539 (HY-15616) (MC1R agonist). MSG606 TFA can inhibit cancer cell proliferation and transition from the G1 to the S phase. MSG606 TFA can delay pain hypersensitivity and reduce cholesterol levels. MSG606 TFA can be used for the researches of cancer, inflammation, neurological and metabolic disease, such as breast cancer and subarachnoid hemorrhage (SAH).
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- Formule: C62H82N20O13S.xC2HF3O2
- Masse moléculaire:1347.51 (free base)
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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MC1R |
MSG606 TFA (20 μM, 3 h) attenuates the NDP-MSH-stimulated increase in cAMP in T-47d and MCF7 cells[3].
MSG606 TFA (20 μM, 6 h) inhibits cell proliferation in NDP-MSH-stimulated T-47d and MCF7 cells[3].
MSG606 TFA (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 TFA (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 TFA () inhibits the mRNA expression of IL-1β and TNFα in LPS ()-stimulated BMDMs[4].
MSG606 TFA (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 TFA (7.5 μg, i.c.v) increases hyperalgesia latencies in Morphine-treated female mice[2].
MSG606 TFA (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.
Chemical Information
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Appearance Solid
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Masse moléculaire 1347.51 (free base)
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Formule C62H82N20O13S.xC2HF3O2
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Color White to off-white
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Sequence Shortening
{Bua}GH-{d-Phe}-R-{d-Trp}-CDRFG-NH2 (Carba sulfide bridge:Bua1-Cys7)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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 Jan;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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MSG606 TFA Related Classifications
HY-P1726A Related Classifications
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