GnRH Receptor Antagonist

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.

Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC₅₀ of 1.21 nM.

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.

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.

Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

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.

Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.

Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.

Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea.

BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC₅₀s of 21 and 24 nM for human and rat GnRH-R, respectively.

Acyline TFA, a GnRH peptide analogue, is a GnRH antagonist that inhibits gonadotropin and testosterone (T) levels.

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.

Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity.

Lumigolix (GnRH antagonist 2) (formula I) is a GnRH receptor antagonist that can be used for endometriosis research.

Degarelix acetate (FE 200486) is a decapeptide that shows high affinity/selectivity to human gonadotropin-releasing hormone (GnRH) receptor (IC₅₀ = 3 nM). Degarelix acetate (FE 200486) is used for the research of prostate cancer.

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.

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC₅₀ value of 0.79 nM, a K_i 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.

Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.

AG-045572 is a GnRH receptor antagonist with K_is of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone.