Home Endocrinology & Hormones GNRH Receptor antagonist Relugolix For research use only.

Relugolix

Synonyms: RVT-601, TAK-385

Relugolix (RVT-601, TAK-385) is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.

Relugolix Chemical Structure

Relugolix Chemical Structure

CAS: 737789-87-6

Purity & Quality Control

Batch: S580801 DMSO] 61 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.76%
99.76

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Biological Activity

Description Relugolix (RVT-601, TAK-385) is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.
Targets
monkey GnRHR [2]
(Cell-free assay)		 human GnRHR [2]
(Cell-free assay)
0.32 nM 0.33 nM
In vitro
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
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].
Animal Research Animal Models Six-week-old male hGNRHR-knock-in mice
Dosages 3, 10 or 30 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06130995 Not yet recruiting
Androgen Deprivation Therapy|Locally Advanced Prostate Cancer
University of Oklahoma
 January 2024 Phase 1
NCT05679388 Recruiting
Prostate Cancer|Prostate Cancer Metastatic|Prostate Adenocarcinoma
University of Chicago
 February 13 2023 Phase 1
NCT04756037 Recruiting
Contraception
Myovant Sciences GmbH
 March 18 2021 Phase 3

Chemical Information & Solubility

Molecular Weight 623.63 Formula

C29H27F2N7O5S
CAS No. 737789-87-6 SDF --
Smiles CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 61 mg/mL ( (97.81 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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

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