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GPCR/G Protein GNRH Receptor Relugolix

Relugolix

Catalog No. T3630   CAS 737789-87-6
Synonyms: TAK-385, RVT-601
Purity 98.85% Datasheet

Relugolix is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

Relugolix, CAS 737789-87-6
Pack Size Availability Price/USD Quantity
1 mg In stock 60.00
5 mg In stock 110.00
10 mg In stock 180.00
25 mg In stock 360.00
50 mg In stock 468.00
1 mL * 10 mM (in DMSO) In stock 180.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Relugolix is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.
Targets&IC50 GNRHR,  
Synonyms TAK-385 , RVT-601
Purity 98.64%
Molecular Weight 623.63
Formula C29H27F2N7O5S
CAS No. 737789-87-6

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 55 mg/mL (88.2 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. MacLean DB et al. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. 2. Nakata D et al. Eur J Pharmacol. 2014 Jan 15;723:167-74.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Neuronal Signaling Compound Library GPCR Compound Library Anti-cancer Clinical Compound Library Fluorochemical Library

Related Products

Related compounds with same targets
Degarelix Danazol Relugolix Goserelin acetate Leuprorelin Leuprolide Acetate Elagolix sodium Cetrorelix

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