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Relugolix (TAK-385, RVT-601) GNRH Receptor antagonist

Name: Relugolix (TAK-385, RVT-601)
Brand: Selleck Chemicals
SKU: S5808
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S5808

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 (TAK-385, RVT-601) GNRH Receptor antagonist Chemical Structure

Quality Control

Batch: Purity: 99.76%

99.76

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR
Other GNRH Receptor Inhibitors	Cetrotide Antide

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (97.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (8.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.5mg/ml (0.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	623.63	Formula	C₂₉H₂₇F₂N₇O₅S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	737789-87-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RVT-601, TAK-385			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

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	monkey GnRHR (Cell-free assay) 0.32 nM human GnRHR (Cell-free assay) 0.33 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).
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.
References	[1] https://academic.oup.com/annonc/article/27/suppl_6/734P/2799472 [2] https://pubmed.ncbi.nlm.nih.gov/24333551/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-17)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04513717	ACTIVE_NOT_RECRUITING	Prostate Adenocarcinoma; Stage III Prostate Cancer AJCC v8; Stage IVA Prostate Cancer AJCC v8	NRG Oncology	2021-01-21	PHASE3
NCT04423211	RECRUITING	Biochemically Recurrent Prostate Carcinoma; Metastatic Prostate Carcinoma; Prostate Adenocarcinoma; Stage IVB Prostate Cancer AJCC v8	ECOG-ACRIN Cancer Research Group	2020-10-08	PHASE3
NCT06378866	RECRUITING	Recurrent Castration-Sensitive Prostate Carcinoma; Recurrent Prostate Cancer; Castration-resistant Prostate Cancer; Biochemically Recurrent Prostate Carcinoma	Mayo Clinic	2024-06-03	PHASE2
NCT06499870	RECRUITING	Prostate Adenocarcinoma	Sean Sachdev	2024-09-06	PHASE2
NCT07216248	RECRUITING	Metastatic Hormone-sensitive Prostate Cancer (mHSPC)	University of Utah	2025-10-27	PHASE2
NCT06397703	RECRUITING	Prostate Cancer	NYU Langone Health	2024-04-16	PHASE2

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