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Degarelix

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Catalog No. T10988Cas No. 214766-78-6

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

Degarelix

Degarelix

😃Good
Catalog No. T10988Cas No. 214766-78-6
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
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50 mg$8477-10 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 Weight1632.26
FormulaC82H103ClN18O16
Cas No.214766-78-6
Relative Density.1.325 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 25 mg/mL (15.32 mM), Sonication is recommended.
DMSO: 10 mg/mL (6.13 mM), Sonication is recommended.
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM0.6126 mL3.0632 mL6.1265 mL30.6324 mL
5 mM0.1225 mL0.6126 mL1.2253 mL6.1265 mL
H2O
1mg5mg10mg50mg
10 mM0.0613 mL0.3063 mL0.6126 mL3.0632 mL

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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:
TargetMol | Animal experimentsFor 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 DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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2 Enter the in vivo formulation:
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