Relugolix

Catalog No.S5808 Synonyms: RVT-601, TAK-385

Relugolix Chemical Structure

Molecular Weight(MW): 623.63

Relugolix is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with an IC50 of 0.12 nM.

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Biological Activity

Description Relugolix is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with an IC50 of 0.12 nM.
In vitro

Relugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM)[2].

In vivo TAK-385 acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis[2].

Protocol

Animal Research:

[2]

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  • Animal Models: Six-week-old male hGNRHR-knock-in mice
  • Formulation: 0.5% methylcellulose solution containing 6 mg/mL citric acid monohydrate
  • Dosages: 3, 10 or 30 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (97.81 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 623.63
Formula

C29H27F2N7O5S

CAS No. 737789-87-6
Storage powder
in solvent
Synonyms RVT-601, TAK-385

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03085095 Recruiting Drug: Relugolix|Drug: Leuprolide Acetate Prostate Cancer Myovant Sciences GmbH April 18 2017 Phase 3
NCT02792062 Completed Drug: TAK-385 40 mg Japanese Premenopausal Healthy Adult Women Takeda July 4 2016 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Estrogen/progestogen Receptor Signaling Pathway Map

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