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Relugolix

Name: Relugolix
Brand: TargetMol
SKU: T3630
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T3630Cas No. 737789-87-6

Alias TAK-385, RVT-601

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.

Relugolix

🥰Excellent

Purity: 99.97%

Catalog No. T3630Alias TAK-385, RVT-601Cas No. 737789-87-6

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	In Stock	In Stock
5 mg	$56	In Stock	In Stock
10 mg	$89	In Stock	In Stock
25 mg	$179	In Stock	In Stock
50 mg	$278	In Stock	In Stock
100 mg	$453	In Stock	In Stock
200 mg	$651	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$78	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.97%

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COA HNMR LCMS

Product Introduction

Bioactivity

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 (R806Q mutations):113 nM, TNK2 (D163E mutations):38nM
Synonyms	TAK-385, RVT-601

Chemical Properties

Molecular Weight	623.63
Formula	C₂₉H₂₇F₂N₇O₅S
Cas No.	737789-87-6
Smiles	CONC(=O)Nc1ccc(cc1)-c1sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccc(OC)nn3)c(=O)c2c1CN(C)C
Relative Density.	1.442 g/cm3 (Predicted)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

keep away from moisture,keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (400.88 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (1.6 mM), Sonication is recommeded.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6035 mL	8.0176 mL	16.0351 mL	80.1757 mL
5 mM	0.3207 mL	1.6035 mL	3.2070 mL	16.0351 mL
10 mM	0.1604 mL	0.8018 mL	1.6035 mL	8.0176 mL
20 mM	0.0802 mL	0.4009 mL	0.8018 mL	4.0088 mL
50 mM	0.0321 mL	0.1604 mL	0.3207 mL	1.6035 mL
100 mM	0.0160 mL	0.0802 mL	0.1604 mL	0.8018 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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

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