Relugolix-d6

CAT: 0804-HY-16474SSize: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-16474SSize:1 mg
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Description
Relugolix-d6 is deuterium labeled 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 Name Alternative
TAK-385-d6
UNSPSC
12352005
Target
GnRH Receptor; Isotope-Labeled Compounds
Type
Isotope-Labeled Compounds
Related Pathways
GPCR/G Protein; Others
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Cancer; Endocrinology
Purity
98.82
Solubility
10 mM in DMSO
Smiles
O=C(NOC)NC1=CC=C(C(S2)=C(CN(C([2H])([2H])[2H])C([2H])([2H])[2H])C(C(N3C4=NN=C(OC)C=C4)=O)=C2N(CC5=C(F)C=CC=C5F)C3=O)C=C1
Molecular Formula
C29H21D6F2N7O5S
Molecular Weight
629.67
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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.|[3]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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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