Relugolix

CAT: 0804-HY-16474-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-16474-01Size:5 mg
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched

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