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Degarelix acetate(214766-78-6 free base)

Catalog No. T10988LCas No. 934016-19-0

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

Degarelix acetate(214766-78-6 free base)

Degarelix acetate(214766-78-6 free base)

Purity: 98.66%
Catalog No. T10988LCas No. 934016-19-0
Degarelix acetate is a competitive and reversible antagonist of gonadotropin-releasing hormone receptor (GnRHR) .
Pack SizePriceAvailabilityQuantity
1 mg$70In Stock
2 mg$100In Stock
5 mg$168In Stock
10 mg$280In Stock
25 mg$503In Stock
50 mg$732In Stock
100 mg$987In Stock
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Purity:98.66%
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Product Introduction

Bioactivity
Description
Degarelix acetate is a competitive and reversible antagonist of gonadotropin-releasing hormone receptor (GnRHR) .
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 Weight1692.34
FormulaC84H107ClN18O18
Cas No.934016-19-0
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
DMSO: 16.92 mg/mL (10 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.5909 mL2.9545 mL5.9090 mL29.5449 mL
5 mM0.1182 mL0.5909 mL1.1818 mL5.9090 mL
10 mM0.0591 mL0.2954 mL0.5909 mL2.9545 mL

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