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

GHSR1a Antagonist

GHSR1a Antagonists (4):

Cat. No. Product Name Effect Purity
  • HY-P5645
    LEAP-2
    		Antagonist
    LEAP-2 (Human liver expressed antimicrobial peptide-2) is a GHS-R1a antagonist, with an IC50 of 6.0 nM. LEAP-2 suppresses the orexigenic effect of ghrelin. LEAP-2 attenuates ghrelin-induced growth hormone (GH) release and reduces basal food intake. LEAP-2 exhibits antimicrobial activity against microbial model organisms. LEAP-2 can be used for the study of obesity and infection.
  • HY-P1139
    Cortistatin-8
    		Antagonist 98.86%
    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.
  • HY-129287
    JMV 3008
    		Antagonist
    JMV 3008 is a GHS-R1a antagonist with an IC50 of 5.6 nM. JMV 3008 can be used in the research of diseases such as diabetes and obesity.