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

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.

MSG606 TFA (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 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.

1347.51 (free base)

C₆₂H₈₂N₂₀O₁₃S.xC₂HF₃O₂

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.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]