Free shipping on all orders over $ 500

Relugolix

Cat. No. M9197
Relugolix Structure
Synonym:

Orgovyx; TAK-385; RVT-601

Size Price Availability Quantity
5mg USD 119.7  USD133 In stock
10mg USD 188.1  USD209 In stock
50mg USD 659.7  USD733 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98.5%
  • 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 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.

Chemical Information
Molecular Weight 623.63
Formula C29H27F2N7O5S
CAS Number 737789-87-6
Purity >98.5%
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.

Related Estrogen Receptor Products
27-Hydroxycholesterol

27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.

SAR439859 (Amcenestrant)

SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.

4-Hydroxytamoxifen

4-Hydroxytamoxifen is a selective estrogen receptor modulator.

Methylpiperidino pyrazole

Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.

Endoxifen E-isomer hydrochloride

Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.