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

GnRH Receptor

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 (17):

Cat. No. Product Name Effect Purity
  • HY-16168A
    Degarelix
    Antagonist ≥98.0%
    Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
  • HY-16474
    Relugolix
    Antagonist ≥98.0%
    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-P0009A
    Cetrorelix Acetate
    Antagonist 99.69%
    Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  • 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-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-17405
    Alarelin Acetate
    Agonist ≥98.0%
    Alarelin acetate is a synthetic GnRH agonist.
  • 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-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-P0051
    Lecirelin
    Agonist 99.80%
    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-13534
    Abarelix
    Antagonist
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
  • HY-13534A
    Abarelix Acetate
    Antagonist 99.62%
    Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.
  • 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.
  • HY-133080
    BAY-784
    Antagonist
    BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively.
  • HY-P1022A
    Kisspeptin-54(human) TFA
    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.
  • HY-P1022
    Kisspeptin-54(human)
    Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion.
  • HY-P0009B
    Cetrorelix diacetate
    Antagonist
    Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
  • HY-U00289
    opigolix
    Antagonist
    Opigolix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist, used for the research of endometriosis and rheumatoid arthritis.
Isoform Specific Products

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