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

GnRH Receptor Antagonist

GnRH Receptor Antagonists (43):

Cat. No. Product Name Effect Purity
  • 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.
  • 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.
  • 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.
  • 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.
  • 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. .
  • 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.
  • 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. .
  • 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.
  • HY-13534
    Abarelix
    		Antagonist 99.90%
    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.
  • HY-16027A
    Acyline TFA
    		Antagonist 99.87%
    Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels.
  • 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.
  • 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.
  • 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.
  • HY-109532
    Ganirelix acetate
    		Antagonist 98.03%
    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).
  • HY-134864
    GnRH antagonist 2
    		Antagonist 98.58%
    GnRH antagonist 2 (formula I) is a GnRH receptor antagonist that can be used for endometriosis research.
  • HY-P0009
    Cetrorelix
    		Antagonist
    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.
  • HY-144863
    BAY 1214784
    		Antagonist
    BAY 1214784 is a potent, selective, and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R). BAY 1214784 is a spiroindoline derivative compound. BAY 1214784 effectively lowers plasma luteinizing hormone levels by up to 49%, at the same time being associated with low pharmacokinetic variability and good tolerability. BAY 1214784 has the potential for the research of uterine fibroids.
  • 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.
  • HY-152856
    Merigolix
    		Antagonist
    Merigolix is a potent gonadotrophin releasing hormone (GnRH) antagonist.
  • 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.