1. GPCR/G Protein
  2. GNRH Receptor
  3. Relugolix

Relugolix (Synonyms: TAK-385)

Cat. No.: HY-16474 Purity: >98.0%
Handling Instructions

Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.

For research use only. We do not sell to patients.

Relugolix Chemical Structure

Relugolix Chemical Structure

CAS No. : 737789-87-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].

IC50 & Target

IC50: 0.33 nM (human GnRH)
IC50: 0.32 nM (monkey GnRH)[2]

In Vitro

Relugolix exhibits strong binding affinity (IC50=0.32 nM) for the monkey receptor comparable to that for the human receptor (IC50=0.33 nM) while displaying a 30000-fold decrease for the rat receptor (IC50=9800 nM). The antagonistic in vitro activity of TAK-385 with respect to the human receptor (IC90=18 nM) exceeded that for the monkey receptor (IC90=1700 nM) by 95-fold in the presence of 40% serum[1].

In Vivo

Relugolix (oral administration; 1-3 mg/kg; single dose for pharmacokinetic study) exhibits a good pharmacokinetic profile and obvious suppressive effects of circulating LH levels in monkeys at a dose of 1 mg/kg. The pharmacokinetic profile exhibits with 16.0 ng/mL, 2.7 h, and 90.1 ng for Cmax, Tmax, and AUCo, respectively in male cynomolgus monkeys[1].
Relugolix (oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks) significantly decreases the testis weight, and reduces the ventral prostate weight at 3 mg/kg and decreases it to castrate levels at 10 mg/kg in male hGNRHR-knock-in mice[2].
Relugolix (oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks) induces constant diestrous phases in all mice within the first week at 100 mg/kg, and significantly decreases the weights of ovaries and uteri at this dose after 4 weeks in female hGNRHR-knock-in mice[2].

Animal Model: Male hGNRHR-knock-in mice[2]
Dosage: 3, 10 or 30 mg/kg
Administration: Oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks
Result: Decreased testicular function.
Animal Model: Female hGNRHR-knock-in mice[2]
Dosage: 30, 100 or 200 mg/kg
Administration: Oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks
Result: Suppressed the hypothalamic–pituitary–gonadal axis to gonadectomized levels.
Downregulated GnRH receptor mRNA levels in the pituitary.
Clinical Trial
Molecular Weight

623.63

Formula

C₂₉H₂₇F₂N₇O₅S

CAS No.

737789-87-6

SMILES

O=C(NOC)NC1=CC=C(C(S2)=C(CN(C)C)C(C(N3C4=NN=C(OC)C=C4)=O)=C2N(CC5=C(F)C=CC=C5F)C3=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (80.18 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6035 mL 8.0176 mL 16.0351 mL
5 mM 0.3207 mL 1.6035 mL 3.2070 mL
10 mM 0.1604 mL 0.8018 mL 1.6035 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

RelugolixTAK-385TAK385TAK 385GNRH ReceptorGonadotropin releasing hormone receptorGNRHRendometriosisuterine fibroidprostate cancerGnRHantagonisticLHFSHInhibitorinhibitorinhibit

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Relugolix
Cat. No.:
HY-16474
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