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-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-P5762
    Phoenixin-14
    99.57%
    Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia.
    Phoenixin-14
  • HY-16027A
    Acyline TFA
    Antagonist 99.87%
    Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels.
    Acyline TFA
  • HY-100209
    Sufugolix
    ≥98.0%
    Sufugolix (TAK-013) is a highly potent and orally available luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC50 of 0.1 nM.
    Sufugolix
  • HY-P1174
    GnRH Associated Peptide (GAP) (1-13), human
    98.60%
    GnRH Associated Peptide (GAP) (1-13), human is an amino acid peptide fragment derived from GnRH. GAP can increase the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in rat anterior pituitary cells. GAP also inhibit the secretion of prolactin.
    GnRH Associated Peptide (GAP) (1-13), human
  • HY-130248B
    (R)-BAY-899
    99.89%
    (R)-BAY-899 is the R-enantiomer of BAY-899. 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.
    (R)-BAY-899
  • HY-19464
    Org 43553
    Agonist 99.30%
    Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.
    Org 43553
  • HY-109532
    Ganirelix acetate
    Antagonist 99.19%
    Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS).
    Ganirelix acetate
  • HY-P1520A
    Prolactin Releasing Peptide (1-31), human acetate
    98.13%
    Prolactin Releasing Peptide (1-31), human (acetate) is a high affinity GPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis.
    Prolactin Releasing Peptide (1-31), human acetate
  • HY-109093
    Linzagolix
    Antagonist 99.68%
    Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research.
    Linzagolix
  • HY-P3582A
    sGnRH-A acetate
    Agonist 99.87%
    sGnRH-A acetate is a salmon gonadotropin-releasing hormone (GnRH) analogue. sGnRH-A acetate stimulates growth hormone secretion. sGnRH-A acetate also can be used as an inducer of ovulation by artificial insemination.
    sGnRH-A acetate
  • HY-13534A
    Abarelix Acetate
    Antagonist 99.89%
    Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.
    Abarelix Acetate
  • HY-P1022A
    Kisspeptin-54(human) TFA
    98.86%
    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.
    Kisspeptin-54(human) TFA
  • HY-W041308
    DCOIT
    Agonist 99.74%
    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.
    DCOIT
  • HY-13699
    NBI-42902
    Antagonist 98.65%
    NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
    NBI-42902
  • HY-P1520
    Prolactin Releasing Peptide (1-31), human
    99.51%
    Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis.
    Prolactin Releasing Peptide (1-31), human
  • HY-P1905
    [Gln8]-C517 (LH-RH), chicken
    Agonist 99.81%
    [Gln8]-C517 (LH-RH), chicken is an avian hypothalamic peptide, which stimulates release of gonadotropins from anterior pituitary, thus regulating reproductive functions.
    [Gln8]-C517 (LH-RH), chicken
  • HY-139303
    LUF5771
    Inhibitor 99.49%
    LUF5771 is a potent allosteric recombinant luteinizing hormone (recLH) and Org 43553 inhibitor. LUF5771 is able to partially activate the LH receptor with low efficacy.
    LUF5771
  • 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-P4534
    (D-His2,D-Trp6)-LHRH
    (D-His2,D-Trp6)-LHRH ((D-His2)-Triptorelin) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development.
    (D-His2,D-Trp6)-LHRH
Cat. No. Product Name / Synonyms Application Reactivity