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Degarelix
Catalog No. T10988Cas No. 214766-78-6
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
Degarelix
Catalog No. T10988Cas No. 214766-78-6
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 50 mg | $847 | 7-10 days |
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Product Introduction
Bioactivity
Chemical Properties
| 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. |
| 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 | 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
H2O
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(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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