GPS1573
Nle-P-f-R-w-FKAVGKKRR-Lys(Nle-P-f-R-w-FKAVGKKRR-)-amide
Where lower case lettering denotes d-amino acids
Where Nle is norleucine
Description
Application Data
Description
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GPS1573 is a potent and dose-dependent peptide antagonist of adrenocorticotrophic (ACTH) -stimulated melanocortin type 2 receptor (MC2R). The binding of ACTH to MC2R regulates steroidogenesis and can lead to metabolic diseases such as Cushing’s disease.
Application Data
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Data Sheet Material Safety Data Sheet (MSDS)Catalogue number crb1000575 Molecular Weight 3685.3 Sequence (one letter code) Nle-P-f-R-w-FKAVGKKRR-Lys(Nle-P-f-R-w-FKAVGKKRR-)-amide
Where lower case lettering denotes d-amino acids
Where Nle is norleucineSequence (three letter code) H-nLeu-Pro-dPhe-Arg-dTrp-Phe-Lys-Ala-Val-Gly-Lys-Lys-Arg-Arg-Lys(nLeu-Pro-dPhe-Arg-dTrp-Phe-Lys-Ala-Val-Gly-Lys-Lys-Arg-Arg)-OH
Purity >95% Storage -20°C References Bouw et al (2014) Development of potent selective competitive-antagonists of the melanocortin type 2 receptor. Mol. cell. endocrinol. 394 99 PMID: 25017734
Manufactured in: United Kingdom GPS1573 is a potent and dose-dependent peptide antagonist of adrenocorticotrophic (ACTH) -stimulated melanocortin type 2 receptor (MC2R). Along with GPS1574, GPS1773 is an ACTH analogue and as such antagonises MC2R in the nanomolar range.
The clinical relevance of GPS1573 is related to Cushing’s disease and syndrome, which are both associated with a hypercortisolemic state. Selective antagonism of MC2R using GPS1573 may be a novel treatment modality for Cushing’s disease and syndrome.