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

GnRH Receptor

Gonadotropin releasing hormone receptor; GNRHR

GnRH Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14369R
    Elagolix sodium (Standard)
    		Antagonist
    Elagolix sodium (Standard) is the analytical standard of Elagolix sodium. This product is intended for research and analytical applications. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
    Elagolix sodium (Standard)
  • HY-17405R
    Alarelin Acetate (Standard)
    		Agonist
    Alarelin (Acetate) (Standard) is the analytical standard of Alarelin (Acetate). This product is intended for research and analytical applications. Alarelin acetate is a synthetic GnRH agonist.
    Alarelin Acetate (Standard)
  • HY-P0009S1
    Cetrorelix-d10
    		Antagonist
    Cetrorelix-d10 (SB-75-d10) is deuterium labeled Cetrorelix. Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist. Cetrorelix inhibits the endogenous luteinizing hormone surge during ovarian stimulation. Cetrorelix reduces cyclophosphamide induced ovarian follicular destruction in mice.
    Cetrorelix-d<sub>10</sub>
  • HY-117982
    SKI2496
    		Antagonist
    SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders.
    SKI2496
  • HY-16474R
    Relugolix (Standard)
    		Antagonist
    Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. 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.
    Relugolix (Standard)
  • HY-106043
    Lutrelin
    		Agonist
    Lutrelin (Wy 40972) is a luteinizing hormone releasing hormone (LHRH) agonist. Lutrelin inhibits the growth of the endometrial expiant in rats.
    Lutrelin
  • HY-164032
    Dimethandrolone undecanoate
    		Inhibitor
    Dimethandrolone undecanoate (7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate) exhibits withrogens and progesterone activity. Dimethandrolone undecanoate inhibits production of gonadotropins, suppresses testosterone production, and thus inhibits sperm production. Dimethandrolone undecanoate is potent for development of male hormone contraceptives.
    Dimethandrolone undecanoate
  • HY-13673S1
    Goserelin-d7
    		Agonist
    Goserelin-d7 (ICI 118630-d7) is deuterium labeled Goserelin. 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-d<sub>7</sub>
  • HY-14789R
    (R)-Elagolix (Standard)
    		Antagonist
    (R)-Elagolix (Standard) is the analytical standard of (R)-Elagolix. This product is intended for research and analytical applications. Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
    (R)-Elagolix (Standard)
  • HY-125701
    A-76154
    		Antagonist
    A-76154, an octapeptide, is a potent reduced-size luteinizing hormone-releasing hormone (LHRH) antagonist.
    A-76154
  • HY-P2357
    MI-1544
    		Antagonist
    MI-1544 is a powerful GnRH antagonist. MI-1544 induces inhibitory effects on the pituitary LH release and on gonads. MI-1544 can be used for the research of antifertility effect.
    MI-1544
  • HY-P2028
    BIM 21009
    		Antagonist
    BIM 21009 is a LHRH and GnRH receptor antagonist. BIM 21009 inhibits tumor growth.
    BIM 21009
  • HY-P0013A
    Antide acetate
    		Inhibitor
    Antide (D-21074) acetate is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
    Antide acetate
  • HY-13673S2
    Goserelin-d7 TFA
    		Agonist
    Goserelin-d7 (TFA) is deuterium labeled Goserelin. 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-d<sub>7</sub> TFA
  • HY-W751574
    Elagolix-d6 sodium
    		Antagonist
    Elagolix-d6 (sodium) (NBI-56418-d6 (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .
    Elagolix-d<sub>6</sub> sodium
  • HY-107533
    T-98475
    T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.2 nM.
    T-98475
  • HY-U00289
    Opigolix
    		Antagonist
    Opigolix (ASP-1707) is a Gonadotropin-releasing hormone (GnRH) receptor antagonist, used for the research of endometriosis and rheumatoid arthritis.
    Opigolix
Cat. No. Product Name / Synonyms Application Reactivity