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

GHSR Antagonist

GHSR Antagonists (10):

Cat. No. Product Name Effect Purity
  • HY-U00433
    JMV 2959
    Antagonist 99.91%
    JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
  • HY-U00433A
    JMV 2959 hydrochloride
    Antagonist 98.09%
    JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32±3 nM in LLC-PK1 cells.
  • HY-13964A
    YIL781 hydrochloride
    Antagonist 99.65%
    YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
  • 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-113906
    GSK1614343
    Antagonist
    GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models.
  • HY-137061
    AZ-GHS-22
    Antagonist
    AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM).
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA
    Antagonist
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-P1432
    K-(D-1-Nal)-FwLL-NH2
    Antagonist
    K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity.
  • HY-13964
    YIL781
    Antagonist 99.68%
    YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively.
  • HY-113906A
    (αR,8aS)-GSK1614343
    Antagonist 99.40%
    (αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06.