HS014 TFA is a potent and selectivemelanocortin-4 (MC4) receptorantagonist, withK_is of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA modulates the behavioral effects of morphine in mice. HS014 TFA increases food intake in free-feeding rats^[1][2][3].

The dose-effect curve of morphine for locomotor activity was shifted downwards in C57Bl/6 mice pretreated with HS014 TFA and in A(y) mice. The dose-effect curve of morphine for antinociception is shifted two- and threefold to the left in C57Bl/6 mice pretreated with HS014 TFA and in A(y) mice, respectively^[2].
Pretreatment with HS014 TFA blocks the effect of IL-1beta on food intake and respiratory exchange ratio (RER) at later time points (beyond 8 h post injection), as well as the hypoactivity and increases metabolic rate^[4].

1677.78

Solid

C₇₃H₉₅F₃N₂₀O₁₉S₂

Ac-Cys-Glu-His-{D-2Nal}-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (Disulfide bridge:Cys1-Cys8)

Ac-CEH-{D-2Nal}-RWGCPPKD-NH2 (Disulfide bridge:Cys1-Cys8)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

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