1. Signaling Pathways
  2. GPCR/G Protein
  3. GHSR
  4. GHSR1a Isoform
  5. GHSR1a Antagonist

GHSR1a Antagonist

GHSR1a Antagonists (2):

Cat. No. Product Name Effect Purity
  • HY-P1139
    Cortistatin-8
    Antagonist
    Cortistatin-8 (CST-8; PCFWKTCK), a neuropeptide, is a GHS-R1a antagonist by counteracting the response of ghrelin on gastric acid secretion. Cortistatin-8 can modulate GH release from somatotroph cells. Cortistatin-8 is a synthetic CST-analogue devoid of any binding affinity to SST-R but capable to bind the GHS-R1a. Cortistatin-8 can exert antagonistic effects on ghrelin actions either in vitro or in vivo in animals.
  • HY-116625
    PF-04628935
    Antagonist
    PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research.