1. GPCR/G Protein
  2. GNRH Receptor

Relugolix (Synonyms: TAK-385)

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

Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.

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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Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013. target: GnRH [1] IC50: 0.33 nM [1] In vivo: In female knock-in mice, twice-daily oral administration of TAK-385 (100mg/kg) induces constant diestrous phases within the first week, decreases the uterus weight to ovariectomized levels and downregulated GnRH receptor mRNA in the pituitary after 4 weeks.[2]

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
References
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Relugolix
Cat. No.:
HY-16474
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Relugolix

Cat. No.: HY-16474