Relugolix

• 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].

• Product Name Alternative:

  TAK-385

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  GnRH Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer; Endocrinology

• Assay Protocol:

  https://www.medchemexpress.com/Relugolix.html

• Purity:

  99.95

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• 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

• Molecular Formula:

  C29H27F2N7O5S

• Molecular Weight:

  623.63

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Kazuhiro Miwa, et al. Discovery of 1-{4-[1- (2,6-Difluorobenzyl) -5-[ (dimethylamino) methyl]-3- (6-methoxypyridazin-3-yl) -2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor. doi/10.1021/jm200216q|[2]Daisuke Nakata, et al. 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. Eur J Pharmacol. 2014 Jan 15;723:167-74.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• CAS Number:

  [737789-87-6]