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 (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-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-16532
    Zoptarelin doxorubicin
    Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro.
    Zoptarelin doxorubicin
  • 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
  • HY-106279
    EA-230
    Ligand 99.92%
    EA-230 is a synthetic oligopeptide originally derived from beta-human chorionic gonadotropin (beta-hCG) lysates. EA-230 has anti-inflammatory effects and can be used for the research of sepsis.
    EA-230
  • HY-16168AS
    Degarelix-d7
    Antagonist
    Degarelix-d7 (FE 200486-d7 free base) is deuterium labeled Degarelix. Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
    Degarelix-d<sub>7</sub>
  • HY-P0056
    Histrelin
    Agonist
    Histrelin, a GnRH analogue, is a GnRH Receptor agonist. Histrelin increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin can be used in the research of prostate cancer, endometriosis.
    Histrelin
  • HY-P3606
    GnRH Associated Peptide (1-24), human
    Activator
    GnRH Associated Peptide (GAP) (1-24), human is the human gonadotropin-releasing hormone-associated peptide (GAP) 1-24 fragment (hGAP-1-24). GAP is joined to the luteinizing hormone-releasing hormone (LH-RH) sequence by a 3 amino acid processing site.
    GnRH Associated Peptide (1-24), human
  • HY-P4568
    (D-Ser4,D-Ser(tBu)6,Azagly10)-LHRH
    (D-Ser4,D-Ser(tBu)6,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-Ser4,D-Ser(tBu)6,Azagly10)-LHRH
  • HY-P3675
    LH-RH (4-10)
    Activator
    LH-RH (4-10) is a heptapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (4-10) produced in macrophages and type II pneumocytes.
    LH-RH (4-10)
  • HY-P3671
    [D-Glp1,D-Phe2,D-Trp3,6]-LH-RH
    Antagonist
    [D-Glp1,D-Phe2,D-Trp3,6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Glp1,D-Phe2,D-Trp3,6]-LH-RH acts as a GnRH receptor antagonist.
    [D-Glp1,D-Phe2,D-Trp3,6]-LH-RH
  • HY-P4693
    (Ser(tBu)6,Azagly10)-LHRH
    (Ser(tBu)6,Azagly10)-LHRH is a potent aza-GLY analog.
    (Ser(tBu)6,Azagly10)-LHRH
  • HY-P3666
    [D-Phe2,6, Pro3]-LH-RH
    [D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist.
    [D-Phe2,6, Pro3]-LH-RH
  • HY-P4144
    Onvitrelin ucalontide
    Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model.
    Onvitrelin ucalontide
  • 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.
    Cetrorelix diacetate
  • HY-P3668
    [D-Lys6]-LH-RH
    Agonist
    [D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist.
    [D-Lys6]-LH-RH
  • HY-W041308R
    DCOIT (Standard)
    Agonist
    DCOIT (Standard) is the analytical standard of DCOIT. This product is intended for research and analytical applications. DCOIT is a representative isothiazolinone that stimulates the gonadotropin-releasing hormone receptor (GnRHR)-mediated synthesis of follicle-stimulating hormone and luteinizing hormone in the brain. DCOIT interferes with G protein-coupled receptors, MAPK and Ca2+ signaling cascades[1].
    DCOIT (Standard)
  • HY-P5762A
    Phoenixin-14 TFA
    Phoenixin-14 (PNX-14) TFA, a BBB-penatrable neuropeptide, has anxiolytic, cardioprotective and neuroprotective effect. Phoenixin-14 TFA can regulate pituitary gonadotrophin secretion by upregulating the GnRH receptor mRNA. Phoenixin-14 TFA stimulates insulin secretion. Phoenixin-14 TFA also protects mice from ischemia/reperfusion (IR) injury. PNX-14 TFA prevents oxidative stress by reducing ROS and increasing GSH.
    Phoenixin-14 TFA
  • HY-P3673
    Lamprey LH-RH I
    Activator
    Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models.
    Lamprey LH-RH I
Cat. No. Product Name / Synonyms Application Reactivity