GnRH Receptor

By Targets:	GnRH Receptor (21) Histamine Receptor (1) Isotope-Labeled Compounds (2) Kisspeptin Receptor (3) Neurokinin Receptor (1) Neuropeptide Y Receptor (1) PERK (1)
By Research Areas:	Cancer (13) Cardiovascular Disease (1) Endocrinology (15) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (5)

Targets Recommended: GnRH Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134864

GnRH antagonist 2

GnRH Receptor Endocrinology

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

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

HY-107534

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

HY-133080

BAY-784

GnRH Receptor Cancer

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 .

BAY-784	GnRH Receptor	Cancer
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 .

HY-105173

Teverelix EP 24332	GnRH Receptor Histamine Receptor	Endocrinology Cancer
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 .

HY-P0056

Histrelin	GnRH Receptor	Cancer
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 .

HY-P0056A

Histrelin acetate	GnRH Receptor	Cancer
Histrelin acetate, a GnRH analogue, is a **GnRH Receptor** agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis .

HY-14369

Elagolix sodium

NBI-56418 sodium
GnRH Receptor Endocrinology Cancer

Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC₅₀ and K_i of 0.25 and 3.7 nM, respectively.

Elagolix sodium NBI-56418 sodium	GnRH Receptor	Endocrinology Cancer
Elagolix sodium is a human **GnRH receptor (GnRHR) antagonist with an IC₅₀ and K_i** of 0.25 and 3.7 nM, respectively.

HY-U00289

Opigolix ASP-1707	GnRH Receptor	Inflammation/Immunology Endocrinology
Opigolix is a Gonadotropin-releasing hormone (GnRH) receptor antagonist, used for the research of endometriosis and rheumatoid arthritis.

HY-P2028

BIM 21009

GnRH Receptor Cancer

BIM 21009 is a LHRH and GnRH receptor antagonist. BIM 21009 inhibits tumor growth .

BIM 21009	GnRH Receptor	Cancer
BIM 21009 is a LHRH and *GnRH* receptor antagonist. BIM 21009 inhibits tumor growth .

HY-P0009A

Cetrorelix Acetate 1 Publications Verification SB-75 acetate	GnRH Receptor	Neurological Disease Endocrinology
Cetrorelix Acetate (SB-75 acetate) is a potent gonadotropin-releasing hormone *(GnRH)* receptor antagonist with an IC₅₀ of 1.21 nM .

HY-P0009B

Cetrorelix diacetate SB-75 diacetate	GnRH Receptor	Neurological Disease Endocrinology
Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone *(GnRH)* receptor antagonist with an IC₅₀ of 1.21 nM .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease
Kisspeptin 13 is a GPR54 and **GnRH receptor** activator, an endogenous active isoform. Kisspeptin 13 enhances memory and can be used in Alzheimer's disease research .

HY-14369S

Elagolix-13C,d3 sodium NBI-56418-¹³C,d₃ sodium	Isotope-Labeled Compounds GnRH Receptor	Endocrinology Cancer
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.

HY-P3668

[D-Lys6]-LH-RH

GnRH Receptor Endocrinology Cancer

[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist .
HY-P3672

[D-Ala6]-LH-RH

GnRH Receptor Endocrinology

[D-Ala6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Ala6]-LH-RH acts as a GnRH receptor agonist .

[D-Lys6]-LH-RH	GnRH Receptor	Endocrinology Cancer
[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a **GnRH receptor** agonist .

[D-Ala6]-LH-RH	GnRH Receptor	Endocrinology
[D-Ala6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Ala6]-LH-RH acts as a **GnRH receptor** agonist .

HY-13699

NBI-42902	GnRH Receptor PERK	Others
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, Ca ²⁺ 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 Ganirest	GnRH Receptor	Metabolic Disease
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-P3862

[MePhe7]-Neurokinin B	Neurokinin Receptor	Neurological Disease Endocrinology
[MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC₅₀ value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R) .

HY-P3671

[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH	GnRH Receptor	Endocrinology
[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 .

HY-16474

Relugolix TAK-385	GnRH Receptor	Endocrinology Cancer
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-P1428

RFRP-1(human)	Neuropeptide Y Receptor	Endocrinology
RFRP-1(human) is a gonadotropin-inhibitory hormone (GnIH) homolog. RFRP-1(human) targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropes and potently inhibits gonadotropin. RFRP-1(human) is a potent Neuropeptide FF (NPFF) receptor agonist with EC50s of 0.0011 nM and 29 nM for NPFF2 and NPFF1, respectively .

HY-16474S

Relugolix-d6 TAK-385-d₆	Isotope-Labeled Compounds GnRH Receptor	Endocrinology Cancer
Relugolix-d₆ is deuterium labeled Relugolix. 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)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].

HY-P5762A

Phoenixin-14 TFA PNX-14 TFA	GnRH Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
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 .

HY-P2161

TAK-683	Kisspeptin Receptor	Cancer
TAK-683 is a potent full *KISS1 receptor* (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀** values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

HY-P2161B

TAK-683 acetate	Kisspeptin Receptor	Cancer
TAK-683 acetate is a potent full *KISS1 receptor* (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀** values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

HY-P2161A

TAK-683 TFA	Kisspeptin Receptor	Cancer
TAK-683 TFA is a potent full *KISS1 receptor* (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀** values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

Cat. No.	Product Name

HY-L047

Endocrinology Compound Library	869 compounds
The endocrine system is a chemical messenger system comprising feedback loops of the hormones released by internal glands of an organism directly into the circulatory system, regulating distant target organs. Hormones are chemicals that serve to communicate between organs and tissues for physiological regulation and behavioral activities. Hormones affect distant cells by binding to specific receptor proteins in the target cell, resulting in a change in cell function. The endocrine system is concerned with the integration of developmental events proliferation, growth, and differentiation, and the psychological or behavioral activities of metabolism, growth and development, tissue function, sleep, digestion, respiration, excretion, mood, stress, lactation, movement, reproduction, and sensory perception caused by hormones. Irregulated hormone release, inappropriate response to signaling or lack of a gland can lead to endocrine disease. MCE offers a unique collection of 869 endocrinology related compounds targeting varieties of hormone receptors such as thyroid hormone receptor, TSH receptor, GNRH receptor, adrenergic receptor, etc. MCE Endocrinology Compound Library is a useful tool for the discovery of endocrinology drugs.

Endocrinology Compound Library

869 compounds

The endocrine system is a chemical messenger system comprising feedback loops of the hormones released by internal glands of an organism directly into the circulatory system, regulating distant target organs. Hormones are chemicals that serve to communicate between organs and tissues for physiological regulation and behavioral activities. Hormones affect distant cells by binding to specific receptor proteins in the target cell, resulting in a change in cell function.

The endocrine system is concerned with the integration of developmental events proliferation, growth, and differentiation, and the psychological or behavioral activities of metabolism, growth and development, tissue function, sleep, digestion, respiration, excretion, mood, stress, lactation, movement, reproduction, and sensory perception caused by hormones. Irregulated hormone release, inappropriate response to signaling or lack of a gland can lead to endocrine disease.

MCE offers a unique collection of 869 endocrinology related compounds targeting varieties of hormone receptors such as thyroid hormone receptor, TSH receptor, GNRH receptor, adrenergic receptor, etc. MCE Endocrinology Compound Library is a useful tool for the discovery of endocrinology drugs.

Cat. No.	Product Name	Target	Research Area

HY-P0056A

Histrelin acetate	GnRH Receptor	Cancer
Histrelin acetate, a GnRH analogue, is a **GnRH Receptor** agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis .

HY-105173

Teverelix EP 24332	GnRH Receptor Histamine Receptor	Endocrinology Cancer
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 .

HY-P0056

Histrelin	GnRH Receptor	Cancer
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 .

HY-P2028

BIM 21009

GnRH Receptor Cancer

BIM 21009 is a LHRH and GnRH receptor antagonist. BIM 21009 inhibits tumor growth .

BIM 21009	GnRH Receptor	Cancer
BIM 21009 is a LHRH and *GnRH* receptor antagonist. BIM 21009 inhibits tumor growth .

HY-P0009B

Cetrorelix diacetate SB-75 diacetate	GnRH Receptor	Neurological Disease Endocrinology
Cetrorelix diacetate (SB-075 diacetate) is a potent gonadotropin-releasing hormone *(GnRH)* receptor antagonist with an IC₅₀ of 1.21 nM .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease
Kisspeptin 13 is a GPR54 and **GnRH receptor** activator, an endogenous active isoform. Kisspeptin 13 enhances memory and can be used in Alzheimer's disease research .

HY-P3668

[D-Lys6]-LH-RH

GnRH Receptor Endocrinology Cancer

[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a GnRH receptor agonist .
HY-P3672

[D-Ala6]-LH-RH

GnRH Receptor Endocrinology

[D-Ala6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Ala6]-LH-RH acts as a GnRH receptor agonist .

[D-Lys6]-LH-RH	GnRH Receptor	Endocrinology Cancer
[D-Lys6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Lys6]-LH-RH acts as a **GnRH receptor** agonist .

[D-Ala6]-LH-RH	GnRH Receptor	Endocrinology
[D-Ala6]-LH-RH is a Luteinizing-hormone-releasing hormone (LHRH) analogue. [D-Ala6]-LH-RH acts as a **GnRH receptor** agonist .

HY-P3862

[MePhe7]-Neurokinin B	Neurokinin Receptor	Neurological Disease Endocrinology
[MePhe7]-Neurokinin B is an neurokinin NK-3 receptor (NK3R) agonist with an IC₅₀ value of 3 nM. [MePhe7]-Neurokinin B is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R) .

HY-P3671

[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH	GnRH Receptor	Endocrinology
[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 .

HY-P1428

RFRP-1(human)	Neuropeptide Y Receptor	Endocrinology
RFRP-1(human) is a gonadotropin-inhibitory hormone (GnIH) homolog. RFRP-1(human) targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropes and potently inhibits gonadotropin. RFRP-1(human) is a potent Neuropeptide FF (NPFF) receptor agonist with EC50s of 0.0011 nM and 29 nM for NPFF2 and NPFF1, respectively .

HY-P5762A

Phoenixin-14 TFA PNX-14 TFA	GnRH Receptor	Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
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 .

HY-P2161

TAK-683	Kisspeptin Receptor	Cancer
TAK-683 is a potent full *KISS1 receptor* (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀** values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

HY-P2161B

TAK-683 acetate	Kisspeptin Receptor	Cancer
TAK-683 acetate is a potent full *KISS1 receptor* (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀** values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

HY-P2161A

TAK-683 TFA	Kisspeptin Receptor	Cancer
TAK-683 TFA is a potent full *KISS1 receptor* (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀** values of 0.96 nM and 1.6 nM for human and rat, respectively . TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer .

Cat. No.	Compare	Product Name	Species	Source

HY-P702298

	GNRHR2 Protein, Rhesus Macaque (Cell-Free, His) Gonadotropin-releasing hormone II Receptor; Type II GnRH Receptor	Rhesus Macaque	E. coli Cell-free
	The GNRHR2 Protein serves as a receptor for gonadotropin-releasing hormone II (GnRH II), initiating its action through association with G proteins that activate a phosphatidylinositol-calcium second messenger system. GNRHR2 Protein, Rhesus Macaque (Cell-Free, His) is the recombinant Rhesus Macaque-derived GNRHR2 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of GNRHR2 Protein, Rhesus Macaque (Cell-Free, His) is 379 a.a., with molecular weight of 44.3 kDa.

Cat. No.	Product Name	Chemical Structure

HY-14369S

Elagolix-13C,d3 sodium
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.

HY-16474S

Relugolix-d6

Relugolix-d₆ is deuterium labeled Relugolix. 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)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].


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