Home Tools
Log in
Cart

Relugolix

Catalog No. T3630   CAS 737789-87-6
Synonyms: RVT-601, TAK-385

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Relugolix Chemical Structure
Relugolix, CAS 737789-87-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
5 mg In stock $ 72.00
10 mg In stock $ 118.00
25 mg In stock $ 209.00
50 mg In stock $ 347.00
100 mg In stock $ 538.00
500 mg In stock $ 1,150.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.67%
Purity: 98.85%
Purity: 98.64%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
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
Synonyms RVT-601, TAK-385
Molecular Weight 623.63
Formula C29H27F2N7O5S
CAS No. 737789-87-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL(88.2 mM)

TargetMolReferences and Literature

1. MacLean DB et al. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. 2. Nakata D et al. Eur J Pharmacol. 2014 Jan 15;723:167-74.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library GPCR Compound Library EMA Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library ReFRAME Related Library FDA-Approved Drug Library

Related Products

Related compounds with same targets
AG 045572 LHRH (R)-Elagolix Goserelin acetate Linzagolix Deslorelin acetate(57773-65-6 free base) Degarelix acetate(214766-78-6 free base) GnRH-R antagonist 1

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Relugolix 737789-87-6 GPCR/G Protein GNRH Receptor inhibit Gonadotropin releasing hormone receptor endometriosis TAK 385 GnRH Receptor GnRH RVT-601 prostate cancer TAK385 GNRHR antagonistic Inhibitor RVT601 uterine fibroid TAK-385 FSH RVT 601 inhibitor

 

TargetMol