Relugolix

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 Specifications

CAS Number

[737789-87-6]

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.