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Relugolix

Relugolix
Relugolix (RVT-601) 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.
Catalog No. T3630Cas No. 737789-87-6
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Purity:99.67%
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Relugolix

Purity: 99.67%
Catalog No. T3630Alias TAK-385, RVT-601Cas No. 737789-87-6

Relugolix (RVT-601) 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.
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Pack SizePriceAvailabilityQuantity
1 mg$31In Stock
5 mg$72In Stock
10 mg$118In Stock
25 mg$209In Stock
50 mg$347In Stock
100 mg$538In Stock
500 mg$1,150In Stock
1 mL x 10 mM (in DMSO)$97In Stock
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Product Introduction

Bioactivity
Description
Relugolix (RVT-601) 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
AliasTAK-385, RVT-601
Chemical Properties
Molecular Weight623.63
FormulaC29H27F2N7O5S
Cas No.737789-87-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (80.18 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6035 mL8.0176 mL16.0351 mL80.1757 mL
5 mM0.3207 mL1.6035 mL3.2070 mL16.0351 mL
10 mM0.1604 mL0.8018 mL1.6035 mL8.0176 mL
20 mM0.0802 mL0.4009 mL0.8018 mL4.0088 mL
50 mM0.0321 mL0.1604 mL0.3207 mL1.6035 mL

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