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 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 (49):

Cat. No. Product Name Effect Purity
  • HY-16168A
    Degarelix
    Antagonist 99.92%
    Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix can be used for prostate cancer research.
  • HY-13673A
    Goserelin acetate
    Agonist 99.89%
    Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
  • HY-P0009A
    Cetrorelix Acetate
    Antagonist 99.85%
    Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  • HY-16474
    Relugolix
    Antagonist 99.67%
    Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.
  • HY-17405
    Alarelin Acetate
    Agonist 99.95%
    Alarelin acetate is a synthetic GnRH agonist.
  • 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.
  • HY-16168B
    Degarelix acetate hydrate
    Antagonist
    Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research.
  • HY-105173
    Teverelix
    Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
  • HY-14369
    Elagolix sodium
    Antagonist 99.66%
    Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
  • HY-P0292
    GnRH-I
    Agonist 98.97%
    GnRH-I is a decapeptide of hypothalamic origin. GnRH-I acts primarily by regulating the release of biologically active follicle stimulating hormone (FSH) and luteinising hormone (LH) from the pituitary site mediated by the GnRH receptor (GnRHR).
  • HY-P0053
    Fertirelin
    99.52%
    Fertirelin is a GnRH and LH-RH analogue; it also becomes the treatment choice for reversing cow follicular cysts.
  • HY-130248
    BAY-899
    99.90%
    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. BAY-899 can reduce sex hormone levels.
  • HY-130249
    BAY-298
    99.94%
    BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels.
  • HY-P0051
    Lecirelin
    Agonist 99.83%
    Lecirelin, a synthetic gonadotropin-releasing hormone (GnRH) analogue, acts as a GnRH agonist. Lecirelin is widely used for the research of bovine ovarian follicular cysts.
  • 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.
  • HY-14789
    (R)-Elagolix
    Antagonist
    Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).
  • HY-13534A
    Abarelix Acetate
    Antagonist 99.61%
    Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.
  • 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.
  • HY-13534
    Abarelix
    Antagonist 99.62%
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
  • 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.