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hormone-dependent diseases

" in MedChemExpress (MCE) Product Catalog:

By Targets:	17β-HSD (3) GnRH Receptor (7) Isotope-Labeled Compounds (1) Progesterone Receptor (1) Reference Standards (1)
By Research Areas:	Cancer (9) Endocrinology (5) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Peptides

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Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-P5897

GnRH antagonist 3	GnRH Receptor	Metabolic Disease
GnRH antagonist 3 (Compound 11) is a GnRH antagonist with an IC₅₀ of 7 nM. GnRH antagonist 3 can be used in the research of hormone-dependent diseases .

HY-16474R

Relugolix (Standard) TAK-385 (Standard)	Reference Standards GnRH Receptor	Endocrinology Cancer
Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. 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-120767

Linzagolix choline KLH-2109 choline; OBE-2109 choline	GnRH Receptor	Inflammation/Immunology Cancer
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-178419

GnRH-R antagonist-3	GnRH Receptor	Cancer
GnRH-R antagonist-3 (Compound 37) is a *Gonadotropin releasing hormone* receptor (GnRH-R) antagonist with IC₅₀*s of 94 and 275 nM for rat and human GnRH-R, respectively. GnRH-R antagonist-3 can be used for hormone dependent* diseases such as endometriosis, breast and prostate cancer research .

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) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .

HY-176270

ESC1002755	17β-HSD	Neurological Disease Cancer
ESC1002755 is a 17β-HSD10 inhibitor with an IC₅₀ of 19 nM. ESC1002755 has significant enzyme specificity with non-/uncompetitive inhibition against the cofactor NADH. ESC1002755 shows minimal cytotoxicity towards the HEK293 at 50 μM. ESC1002755 is promising for Alzheimer’s disease and hormone-dependent cancers (such as prostate, bone and colorectal cancer) research .

HY-W267205

3-Acetyl-7-Hydroxycoumarin	17β-HSD	Endocrinology Cancer
3-Acetyl-7-Hydroxycoumarin (Compound 2) is a high selective 17-beta-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitor. 3-Acetyl-7-Hydroxycoumarin shows a significant improvement of the inhibitory potency, with 57% inhibition of 17β-HSD1 at 6 μM. 3-Acetyl-7-Hydroxycoumarin is promising for research of hormone-dependent diseases, such as breast cancer and endometriosis .

HY-155535

17β-HSD10-IN-2	17β-HSD	Neurological Disease
17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor，targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10)，a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer .

HY-178418

GnRH-R antagonist-2	GnRH Receptor	Cancer
GnRH-R antagonist-2 (Compound 44c) is a *Gonadotropin releasing hormone* receptor (GnRH-R) antagonist with IC₅₀*s of 43 and 88 nM for rat and human GnRH-R, respectively. GnRH-R antagonist-2 can be used for hormone dependent* diseases such as endometriosis, breast and prostate cancer research .

HY-119080

CP8754	Progesterone Receptor	Endocrinology Cancer
CP8754 is an orally active, selective human progesterone receptor (hPR) antagonist that blocks progesterone-mediated signaling pathways. CP8754 competitively inhibits the binding of [ ³H]-progesterone to hPR. And in vitro, CP8754 inhibits progesterone-dependent exogenous luciferase and endogenous alkaline phosphatase expression; while in vivo, CP8754 inhibits rabbit endometrial transformation. CP8754 does not significantly bind to human glucocorticoid receptors (hGR), estrogen receptors (hER), or rat androgen receptors (rAR). CP8754 can be used in the study of progesterone-related diseases such as breast cancer, endometriosis, uterine fibroids, and meningioma, as well as hormone-dependent tumors .

Cat. No.	Product Name	Target	Research Area

HY-P5897

GnRH antagonist 3	GnRH Receptor	Metabolic Disease
GnRH antagonist 3 (Compound 11) is a GnRH antagonist with an IC₅₀ of 7 nM. GnRH antagonist 3 can be used in the research of hormone-dependent diseases .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-155535

17β-HSD10-IN-2	Monophenols Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Phenols Endogenous metabolite Disease Research Fields Source Classification	17β-HSD
17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor，targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10)，a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer .

Cat. No.	Product Name	Chemical Structure

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) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .

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) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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