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-16168A
    Degarelix
    		Antagonist 99.92%
    Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC50 = 3 nM). Degarelix acetate Degarelix acetate (FE 200486) is used for the research of prostate cancer.
    Degarelix
  • HY-P0009A
    Cetrorelix Acetate
    		Antagonist 99.87%
    Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM.
    Cetrorelix Acetate
  • HY-13673A
    Goserelin acetate
    		Agonist 99.92%
    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.
    Goserelin acetate
  • HY-130248
    BAY-899
    		99.93%
    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.
    BAY-899
  • HY-P0053
    Fertirelin
    		99.52%
    Fertirelin is a GnRH and LH-RH analogue. Fertirelin can be used of the study for reversing cow follicular cysts.
    Fertirelin
  • HY-P3641A
    Kisspeptin 13 TFA
    		Activator 99.40%
    Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research.
    Kisspeptin 13 TFA
  • HY-P10419
    Zebrafish Kisspeptin-1
    		Agonist
    Zebrafish Kisspeptin-1 is the core sequence of the neuropeptide kisspeptin-1, which participate in the regulation of gonadotropin-releasing hormone (GnRH) release, and regulates the reproductive system.
    Zebrafish Kisspeptin-1
  • HY-120767
    Linzagolix choline
    		Antagonist
    Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids.
    Linzagolix choline
  • HY-P1022
    Kisspeptin-54(human)
    		98.00%
    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.
    Kisspeptin-54(human)
  • HY-16474
    Relugolix
    		Antagonist 99.95%
    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
  • HY-17405
    Alarelin Acetate
    		Agonist 99.90%
    Alarelin acetate is a synthetic GnRH agonist.
    Alarelin Acetate
  • HY-P0051
    Lecirelin
    		Agonist 99.06%
    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.
    Lecirelin
  • HY-14369
    Elagolix sodium
    		Antagonist 99.94%
    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 sodium
  • HY-P4190
    Fsh receptor-binding inhibitor fragment(bi-10)
    		Antagonist 99.77%
    FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries.
    Fsh receptor-binding inhibitor fragment(bi-10)
  • HY-14789
    (R)-Elagolix
    		Antagonist
    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
  • HY-130249
    BAY-298
    		99.96%
    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.
    BAY-298
  • HY-P0243
    Luteinizing Hormone Releasing Hormone (LH-RH), salmon
    		99.69%
    Luteinizing Hormone Releasing Hormone (LH-RH), salmon (Salmon GnRH) is the hypophysiotropic decapeptide synthesized in the hypothalamus that plays a crucial role in the control of reproductive functions.
    Luteinizing Hormone Releasing Hormone (LH-RH), salmon
  • HY-P0056A
    Histrelin acetate
    		Agonist 99.90%
    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-P0013
    Antide
    		Antagonist 99.86%
    Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
    Antide
  • HY-13534
    Abarelix
    		Antagonist 99.90%
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
    Abarelix
Cat. No. Product Name / Synonyms Application Reactivity