[CAS NO. 737789-87-6] Relugolix

Name: Relugolix
Brand: Arctom Scientific
SKU: SLK-S5808

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PRODUCTS SPECIFICATIONS [737789-87-6]

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Catalog

SLK-S5808

Brand

Selleck

CAS

737789-87-6

DESCRIPTION [737789-87-6]

Overview

MDL	MFCD25976856
Molecular Weight	623.63
Molecular Formula	C29H27F2N7O5S
SMILES	C(N1C2=C(C(CN(C)C)=C(S2)C3=CC=C(NC(NOC)=O)C=C3)C(=O)N(C1=O)C4=CC=C(OC)N=N4)C5=C(F)C=CC=C5F

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	0.0321 mL	0.1604 mL	0.3207 mL

Description

Relugolix (RVT-601, TAK-385) is a selective antagonist of the with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.

Targets

monkey GnRHR ^[2] (Cell-free assay)	human GnRHR ^[2] (Cell-free assay)
0.32 nM	0.33 nM

In vitro

Relugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM).

In vivo

TAK-385 acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis.

References

[1] D. Dearnaley, et al. Annals of Oncology. 2016, 27 (suppl_6):734P.
[2] Nakata D, et al. Eur J Pharmacol. 2014, 723:167-74.

Synonyms

Urea, N-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N′-methoxy-

N-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[(dimethylamino)methyl]-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N′-methoxyurea

TAK 385

Relugolix

1-[4-[1-[(2,6-Difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea

RVT 601

Orgovyx