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Relugolix

Catalog No. T3630 CAS 737789-87-6

Synonyms: RVT-601, TAK-385

Relugolix 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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Relugolix, CAS 737789-87-6

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

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 2 years

Solubility Information

DMSO: 55 mg/mL(88.2 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

Dose Conversion

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

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

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Step Two: Enter the in vivo formulation

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Molarity Calculator

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Molecular Weight Calculator

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Mass of a compound required to prepare a solution of known volume and concentration
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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)
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The answer of 19.713 mg appears in the Mass box

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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.

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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)
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Molecule Formula

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Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
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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.

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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 RVT-601 GnRH Receptor GnRH prostate cancer GNRHR antagonistic Inhibitor TAK385 uterine fibroid FSH TAK 385 TAK-385 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.