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Degarelix (GSK1278863)

Cat. No. M10250
Degarelix (GSK1278863) Structure
Synonym:

FE-200486; GSK1278863

Size Price Availability Quantity
5mg USD 175  USD175 In stock
10mg USD 290  USD290 In stock
25mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

Degarelix (GSK1278863) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. 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. Degarelix (0.3 to 10 μg/kg) in rats produces a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels.

Chemical Information
Molecular Weight 1632.26
Formula C82H103ClN18O16
CAS Number 214766-78-6
Solubility (25°C) DMSO 10 mg/mL
Water 5 mg/mL (ultrasonic and warming)
Storage -20°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Monica Sakai, et al. PLoS One. In search of the molecular mechanisms mediating the inhibitory effect of the GnRH antagonist degarelix on human prostate cell growth

[2] Ferenc G Rick, et al. Onco Targets Ther. An update on the use of degarelix in the treatment of advanced hormone-dependent prostate cancer

[3] Anders Sonesson, et al. Drug Metab Dispos. Metabolite profiles of degarelix, a new gonadotropin-releasing hormone receptor antagonist, in rat, dog, and monkey

[4] Pierre Broqua, et al. J Pharmacol Exp Ther. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: degarelix

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Keywords: Degarelix (GSK1278863), FE-200486; GSK1278863 supplier, LHRH/GnRH, inhibitors, activators


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