MSG606 

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)^[1][2][3][4].

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.

MSG606 (6 nM, i.c.v, 1 h befor SAH) abolishes the anti-inflammation effects of BMS-470539 (HY-15616) in subarachnoid hemorrhage (SAH) rats^[1].
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.

1347.51

C₆₂H₈₂N₂₀O₁₃S

1416983-77-1

Solid

White to off-white

{Bua}GH-{d-Phe}-R-{d-Trp}-CDRFG-NH2 (Carba sulfide bridge:Bua1-Cys7)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

* 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.

• [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]