Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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.
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 | TNK2(D163E mutations):38nM, TNK2(R806Q mutations):113 nM |
Synonyms | RVT-601, TAK-385 |
Molecular Weight | 623.63 |
Formula | C29H27F2N7O5S |
CAS No. | 737789-87-6 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 55 mg/mL(88.2 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Relugolix 737789-87-6 GPCR/G Protein GNRH Receptor inhibit Gonadotropin releasing hormone receptor endometriosis RVT-601 GnRH Receptor GnRH prostate cancer GNRHR antagonistic Inhibitor TAK385 uterine fibroid FSH TAK 385 TAK-385 inhibitor