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-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-152856
    Merigolix
    		Antagonist
    Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist.
    Merigolix
  • HY-16168B
    Degarelix acetate hydrate
    		Antagonist
    Degarelix acetate hydrate (FE 200486 acetate hydrate) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research.
    Degarelix acetate hydrate
  • 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.
    Teverelix
  • 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-P11265
    YQGN-7
    YQGN-7 is a targeted fluorescent probe for the gonadotropin-releasing hormone receptor (RnRHR). YQGN-7 exhibits high selectivity and affinity for breast cancer cells (KD = 217.8 nM). YQGN-7 achieves precise visualization of the primary and metastatic lesions of breast cancer by targeting the highly expressed GnRHR in tumor cells. YQGN-7 can be used in the research of breast cancer breast-conserving surgery (BCS).
    YQGN-7
  • HY-P4564
    (D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH
    (D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH is an analogue of luteinizing hormone-releasing hormone (LHRH). LHRH plays a central role in the control of reproduction by stimulating the release of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
    (D-Ser(tBu)6,D-Leu7,Azagly10)-LHRH
  • HY-178419
    GnRH-R antagonist-3
    		Antagonist
    GnRH-R antagonist-3 (Compound 37) is a Gonadotropin releasing hormone receptor (GnRH-R) antagonist with IC50s of 94 and 275 nM for rat and human GnRH-R, respectively. GnRH-R antagonist-3 can be used for hormone dependent diseases such as endometriosis, breast and prostate cancer research.
    GnRH-R antagonist-3
  • HY-106138
    Avorelin
    		Agonist
    Avorelin (Meterelin) is a gonadotropin releasing hormone (GnRH) agonist. Avorelin can be used of the study of prostate cancer.
    Avorelin
  • HY-P3605
    GnRH Associated Peptide (25-53), human
    		Activator
    GnRH Associated Peptide (GAP) (25-53), human is the human gonadotropin-releasing hormone-associated peptide (GAP) 25-53 fragment (hGAP-25-53), can be used as immunogen to generate antiseras including MC-1, MC-2, and MC-3. GAP is joined to the luteinizing hormone-releasing hormone (LH-RH) sequence by a 3 amino acid processing site.
    GnRH Associated Peptide (25-53), human
  • HY-P2067
    Argtide
    		Antagonist
    Argtide is a luteinizing hormone-releasing hormone (LHRH) antagonist. Argtide is used in endometriosis and cancer-related research.
    Argtide
  • HY-P11278
    Federelin
    Federelin (Gonadorelin[6-D-Phe]) is a gonadotropin (GnRH) analog.
    Federelin
  • HY-P4688
    (Ser(Ac)4,D-Ser(tBu)6,Azagly10)-LHRH
    (Ser(Ac)4,D-Ser(tBu)6,Azagly10)-LHRH is an important peptide hormone.
    (Ser(Ac)4,D-Ser(tBu)6,Azagly10)-LHRH
  • HY-P3583
    (Des-Gly10,D-Arg6,Pro-NHEt9)-LHRH II (chicken)
    Des-Gly10,D-Arg6,Pro-NHEt9)-LHRH II (chicken) is an active petide. (Des-Gly10,D-Arg6,Pro-NHEt9)-LHRH II (chicken) can be used for the research of various biochemical studies.
    (Des-Gly10,D-Arg6,Pro-NHEt9)-LHRH II (chicken)
  • HY-P3975
    Glp-His-Pro-Gly-NH2
    		Agonist
    Glp-His-Pro-Gly-NH2 (pGlu-His-Pro-Gly-NH2) is a peptide containing 4 amino acids. Glp-His-Pro-Gly-NH2 stimulates gonadotrophin, luteinizing hormone (LH) and follicle stimulating hormone (FSH) release.
    Glp-His-Pro-Gly-NH2
  • HY-P4739
    LHRH (1-5) free acid
    LHRH (1-5) (free acid) is a polypeptide generated by the cleavage of LHRH at the Tyr55-Gly66 site. LHRH (1-5) (free acid) is converted into LHRH (1-3) and LHRH (4-5) fragments under the catalysis of Angiotensin-converting enzyme (HY-P2983).
    LHRH (1-5) free acid
  • HY-P3084
    Human follicular gonadotropin releasing peptide
    Human follicular gonadotropin releasing peptide (hF-GRP) is a hormone peptide. Human follicular gonadotropin releasing peptide can stimulate pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion in vitro.
    Human follicular gonadotropin releasing peptide
  • HY-P2446
    ORG 30276
    		Antagonist
    ORG 30276 (APTAA-LHRH) is a potent GnRH antagonist that effectively reduces serum LH and FSH levels in male rats. ORG 30276 significantly decreases unoccupied pituitary GnRH receptors, leading to suppressed gonadotropin secretion. ORG 30276 treatment results in a considerable reduction in mRNA levels of gonadotropin beta-subunits in the pituitary gland. ORG 30276's effects on gonadotropin dynamics can be selectively reversed by the replacement of specific sex steroids, with androgens being particularly effective for the FSH beta-subunit mRNA levels.
    ORG 30276
  • HY-14369S
    Elagolix-13C,d3 sodium
    		Antagonist
    Elagolix-13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
    Elagolix-<sup>13</sup>C,d<sub>3</sub> sodium
  • HY-P10378
    GPR10 agonist 1
    		Agonist
    GPR10 agonist 1 (compound 18-S4) is a potent GPR10 agonist with EC50 values of 80, 7.8 nM in the presence (10%) or absence (0%) of FBS, respectively. GPR10 agonist 1 has the potential for the research of chronic obesity.
    GPR10 agonist 1
Cat. No. Product Name / Synonyms Application Reactivity