1. Signaling Pathways
  2. GPCR/G Protein
  3. GnRH Receptor

GnRH Receptor

Gonadotropin releasing hormone receptor; GNRHR

The GnRH receptor (Gonadotropin-releasing hormone receptor, GNRHR) is a member of the rhodopsin-like G protein-coupled receptor (GPCR) family and consists of seven transmembrane helical domains connected via extra- and intra-cellular segments. GnRH receptor is located on the plasma membrane of gonadotrophs, pituitary cells that synthesize the gonadotrophins LH and FSH.

Mammalian type I and II GnRH receptors show differential ligand preference for GnRH-I (also named as LHRHR) and GnRH-II, respectively. All GnRH receptors activate the Gq/11 family of G proteins, which activate phospholipase C-catalyzed production of second messengers that activate protein kinase C (PKC). GnRH receptor activated by GnRH analogues stimulates the synthesis and release of LH and FSH. GnRH receptors can be used for the research of breast and prostate cancer, regulation of fertility, endometriosis and a range of other medical and veterinary uses.

GnRH Receptor Related Products (94):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-130248B
    (R)-BAY-899
    99.71%
    (R)-BAY-899 is the R-enantiomer of BAY-899. BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively.
    (R)-BAY-899
  • HY-P0056A
    Histrelin acetate
    Agonist 98.83%
    Histrelin acetate, a GnRH analogue, is a GnRH Receptor agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis.
    Histrelin acetate
  • HY-P5762
    Phoenixin-14
    99.57%
    Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia.
    Phoenixin-14
  • HY-P1022A
    Kisspeptin-54(human) TFA
    99.66%
    Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion.
    Kisspeptin-54(human) TFA
  • HY-P1174
    GnRH Associated Peptide (GAP) (1-13), human
    98.60%
    GnRH Associated Peptide (GAP) (1-13), human is an amino acid peptide fragment derived from GnRH. GAP can increase the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in rat anterior pituitary cells. GAP also inhibit the secretion of prolactin.
    GnRH Associated Peptide (GAP) (1-13), human
  • HY-16027A
    Acyline TFA
    Antagonist 99.87%
    Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels.
    Acyline TFA
  • HY-P1520
    Prolactin Releasing Peptide (1-31), human
    Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis.
    Prolactin Releasing Peptide (1-31), human
  • HY-134864
    GnRH antagonist 2
    Antagonist 98.16%
    GnRH antagonist 2 (formula I) is a GnRH receptor antagonist that can be used for endometriosis research.
    GnRH antagonist 2
  • HY-P1808
    LGnRH-III, lamprey
    99.80%
    LGnRH-III, lamprey, an isoform of GnRH isolated from the sea lamprey, is a weak GnRH agonist with antitumor activities.
    LGnRH-III, lamprey
  • HY-13534
    Abarelix
    Antagonist 99.90%
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
    Abarelix
  • HY-P4572
    (D-Trp6)-LHRH free acid
    Agonist 99.97%
    (D-Trp6)-LHRH free acid is a luteinizing hormone-releasing hormone (LHRH) agonist.
    (D-Trp6)-LHRH free acid
  • HY-13699
    NBI-42902
    Antagonist 98.65%
    NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
    NBI-42902
  • HY-109532
    Ganirelix acetate
    Antagonist 98.03%
    Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS).
    Ganirelix acetate
  • HY-P4534
    (D-His2,D-Trp6)-LHRH
    (D-His2,D-Trp6)-LHRH ((D-His2)-Triptorelin) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development.
    (D-His2,D-Trp6)-LHRH
  • HY-P3582
    sGnRH-A
    Agonist
    sGnRH-A is a salmon gonadotropin-releasing hormone (GnRH) analogue. sGnRH-A stimulates growth hormone secretion. sGnRH-A also can be used as an inducer of ovulation by artificial insemination.
    sGnRH-A
  • HY-13673
    Goserelin
    Agonist
    Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
    Goserelin
  • HY-144863
    BAY 1214784
    Antagonist
    BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids.
    BAY 1214784
  • HY-151247
    GnRH-R antagonist 1
    Antagonist
    GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing.
    GnRH-R antagonist 1
  • HY-109093
    Linzagolix
    Antagonist 99.81%
    Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research.
    Linzagolix
  • HY-152856
    Merigolix
    Antagonist
    Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist.
    Merigolix