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Relugolix

Cat. No. M9197
Relugolix Structure
Synonym:

TAK-385; RVT-601

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Relugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM). 

Relugolix (TAK-385) acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Six-week-old male hGNRHR-knock-in mice
Formulation 0.5% methylcellulose solution containing 6 mg/mL citric acid monohydrate
Dosages 3, 10 or 30 mg/kg
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 623.63
Formula C29H27F2N7O5S
CAS Number 737789-87-6
Purity >98%
Solubility DMSO: ≥ 48 mg/mL
Storage at -20°C
References

Medical Castration Using the Investigational Oral GnRH Antagonist TAK-385 (Relugolix): Phase 1 Study in Healthy Males.
MacLean DB, et al. J Clin Endocrinol Metab. 2015 Dec;100(12):4579-87. PMID: 26502357.

Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix), a novel, investigational, orally active, small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice.
Nakata D, et al. Eur J Pharmacol. 2014 Jan 15;723:167-74. PMID: 24333551.

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Keywords: Relugolix, TAK-385; RVT-601 supplier, Estrogen Receptor, inhibitors

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