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Degarelix

Catalog No. T10988Cas No. 214766-78-6

Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.

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.

Pack Size	Price	Availability	Quantity
50 mg	$847	7-10 days

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Product Introduction

Bioactivity

Description	Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
In vitro	Degarelix directly acts on the pituitary receptors to luteinizing hormone-releasing hormone (LHRH), preventing the effect of endogenous LHRH. The use of degarelix eliminates the undesirable surge of initial gonadotropin and testosterone levels produced by LHRH agonists. With the exception of PC-3 cells, Degarelix treatment reduces the cell viability of all prostate cell lines (WPE1-NA22, WPMY-1, BPH-1 cells, VCaP cells). GnRH antagonist degarelix has a direct effect on the growth of prostate cells through apoptosis.
In vivo	In a single subcutaneous injection of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent inhibition of the pituitary-gonad axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. The duration of LH inhibition increased with increasing dose: in rats, after subcutaneous injection of digarelix 12.5, 50 or 200 μg/kg, the significant inhibition of LH lasted 1, 2 and 7 days, respectively [ 3]. Degarelix is stable when incubated in microsomes and liver cells cryopreserved in animal liver tissue.

Chemical Properties

Molecular Weight	1632.26
Formula	C82H103ClN18O16
Cas No.	214766-78-6

Storage & Solubility Information

Storage

keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 25 mg/mL (15.32 mM)

DMSO: 10 mg/mL (6.13 mM)

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	0.6126 mL	3.0632 mL	6.1265 mL	30.6324 mL
5 mM	0.1225 mL	0.6126 mL	1.2253 mL	6.1265 mL

H2O

	1mg	5mg	10mg	50mg
10 mM	0.0613 mL	0.3063 mL	0.6126 mL	3.0632 mL
20 mM	0.0306 mL	0.1532 mL	0.3063 mL	1.5316 mL
50 mM	0.0123 mL	0.0613 mL	0.1225 mL	0.6126 mL
100 mM	0.0061 mL	0.0306 mL	0.0613 mL	0.3063 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% 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 μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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

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