GPS1573 

GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC₅₀=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R^[1].

GPS1573 (0-100 μM; 20 min) antagonizes adrenocorticotropic hormone (ACTH)-stimulated MC2R activity in a dose-dependent manner, with an IC₅₀ of 66 nM^[1].
GPS1573 (0-100 μM; 20 min) antagonizes the activity of α-MSH in HEK293 cells transiently transfected with MC3R, with an IC₅₀ of 460 nM^[1].
GPS1573 (0-100 μM; 20 min) antagonizes the activity of α-MSH in HEK293 cells transiently transfected with MC4R, with an IC₅₀ of 950 nM^[1].
GPS1573 (0-100 μM; 20 min) antagonizes the activity of α-MSH in HEK293 cells transiently transfected with MC5R, with an IC₅₀ of 430 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1788.20

C₈₆H₁₃₈N₂₈O₁₄

2445822-54-6

Solid

White to off-white

{Nle}-Pro-{d-Phe}-Arg-{d-Trp}-Phe-Lys-Ala-Val-Gly-Lys-Lys-Arg-Arg-NH2

{Nle}-P-{d-Phe}-R-{d-Trp}-FKAVGKKRR-NH2

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)

* 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Bouw E, et al. Development of potent selective competitive-antagonists of the melanocortin type 2 receptor. Mol Cell Endocrinol. 2014;394(1-2):99-104.  [Content Brief]