Relugolix | CAS 737789-87-6

Relugolix

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
250mg	$1145	Check With Us
500mg	$1945	Check With Us
1g	$2915	Check With Us

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Cat #: V4596 CAS #: 737789-87-6 Purity ≥ 98%

Description: Relugolix (formerly TAK-385; TAK385; trade names: Orgovyx and Relumina) is a non-peptidyl and orally bioactive antagonist of gonadotropin-releasing hormone (GnRH) approved in 2020 for use in the treatment of prostate cancer in men and uterine fibroids in women.

References: 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 Antagonis

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	623.63
Molecular Formula	C29H27F2N7O5S
CAS No.	737789-87-6
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent

Protocol	In Vitro	Relugolix exhibits strong binding affinity (IC50=0.32 nM) for the monkey receptor comparable to that for the human receptor (IC50=0.33 nM) while displaying a 30000-fold decrease for the rat receptor (IC50=9800 nM). The antagonistic in vitro activity of TAK-385 with respect to the human receptor (IC90=18 nM) exceeded that for the monkey receptor (IC90=1700 nM) by 95-fold in the presence of 40% serum
Protocol	In Vivo	Relugolix (oral administration; 1-3 mg/kg; single dose for pharmacokinetic study) exhibits a good pharmacokinetic profile and obvious suppressive effects of circulating LH levels in monkeys at a dose of 1 mg/kg. The pharmacokinetic profile exhibits with 16.0 ng/mL, 2.7 h, and 90.1 ng for Cmax, Tmax, and AUCo, respectively in male cynomolgus monkeys

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.6035 mL	8.0176 mL	16.0351 mL	32.0703 mL
5mM	0.3207 mL	1.6035 mL	3.2070 mL	6.4141 mL
10mM	0.1604 mL	0.8018 mL	1.6035 mL	3.2070 mL
20mM	0.0802 mL	0.4009 mL	0.8018 mL	1.6035 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.