Relugolix (Synonyms: TAK-385)

Name: Relugolix
Brand: MedChemExpress
SKU: HY-16474
Rating: 4.5 (1 reviews)

Cat. No.: HY-16474 Purity: 99.95%: FAQs
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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). Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al.

For research use only. We do not sell to patients.

Relugolix Chemical Structure

CAS No. : 737789-87-6

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10 mM * 1 mL in DMSO ready for reconstitution	USD 96	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 96	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Relugolix:

Relugolix-d₆ Get quote
Relugolix (Standard) Get quote

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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].

IC₅₀ & Target

IC50: 0.33 nM (human GnRH)
IC50: 0.32 nM (monkey GnRH)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.08 nM Compound: 16b, TAK-385	Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter	[PMID: 21657270]
CHO	IC₅₀	0.32 nM Compound: 16b, TAK-385	Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter	[PMID: 21657270]
CHO	IC₅₀	0.32 nM Compound: 16b, TAK-385	Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum	[PMID: 21657270]
CHO	IC₅₀	0.33 nM Compound: 16b, TAK-385	Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting	[PMID: 21657270]
CHO	IC₅₀	0.33 nM Compound: 16b, TAK-385	Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum	[PMID: 21657270]
CHO	IC₅₀	0.33 nM Compound: 16b, TAK-385	Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum	[PMID: 21657270]
CHO	IC₅₀	0.82 nM Compound: 16b, TAK-385	Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p	[PMID: 21657270]
CHO	IC₅₀	1700 nM Compound: 16b, TAK-385	Antagonist activity at monkey GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in Antagonist activity at monkey GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in	[PMID: 21657270]
CHO	IC₅₀	18 nM Compound: 16b, TAK-385	Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in p	[PMID: 21657270]
CHO	IC₅₀	9800 nM Compound: 16b, TAK-385	Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter Displacement of [125I]leuprorelin from monkey GnRH receptor expressed in CHO cells after 60 mins by X-ray counter	[PMID: 21657270]

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max, T_max, and AUC_o, respectively in male cynomolgus monkeys^[1].
Relugolix (oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks) significantly decreases the testis weight, and reduces the ventral prostate weight at 3 mg/kg and decreases it to castrate levels at 10 mg/kg in male hGNRHR-knock-in mice^[2].
Relugolix (oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks) induces constant diestrous phases in all mice within the first week at 100 mg/kg, and significantly decreases the weights of ovaries and uteri at this dose after 4 weeks in female hGNRHR-knock-in mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male hGNRHR-knock-in mice^[2]
Dosage:	3, 10 or 30 mg/kg
Administration:	Oral administration; 3, 10 or 30 mg/kg; twice daily; 4 weeks
Result:	Decreased testicular function.

Animal Model:	Female hGNRHR-knock-in mice^[2]
Dosage:	30, 100 or 200 mg/kg
Administration:	Oral administration; 30, 100 or 200 mg/kg; twice daily; 4 weeks
Result:	Suppressed the hypothalamic–pituitary–gonadal axis to gonadectomized levels. Downregulated GnRH receptor mRNA levels in the pituitary.

Clinical Trial

Molecular Weight

623.63

Formula

C₂₉H₂₇F₂N₇O₅S

CAS No.

737789-87-6

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (160.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (1.33 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (1.33 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.83 mg/mL (1.33 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (250 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6035 mL	8.0176 mL	16.0351 mL	40.0879 mL
	5 mM	0.3207 mL	1.6035 mL	3.2070 mL	8.0176 mL
	10 mM	0.1604 mL	0.8018 mL	1.6035 mL	4.0088 mL
	15 mM	0.1069 mL	0.5345 mL	1.0690 mL	2.6725 mL
	20 mM	0.0802 mL	0.4009 mL	0.8018 mL	2.0044 mL
	25 mM	0.0641 mL	0.3207 mL	0.6414 mL	1.6035 mL
	30 mM	0.0535 mL	0.2673 mL	0.5345 mL	1.3363 mL
	40 mM	0.0401 mL	0.2004 mL	0.4009 mL	1.0022 mL
	50 mM	0.0321 mL	0.1604 mL	0.3207 mL	0.8018 mL
	60 mM	0.0267 mL	0.1336 mL	0.2673 mL	0.6681 mL
	80 mM	0.0200 mL	0.1002 mL	0.2004 mL	0.5011 mL
	100 mM	0.0160 mL	0.0802 mL	0.1604 mL	0.4009 mL

Relugolix Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Relugolix737789-87-6TAK-385TAK385TAK 385GnRH ReceptorGonadotropin releasing hormone receptorGNRHRendometriosisuterine fibroidprostate cancerGnRHantagonisticLHFSHInhibitorinhibitorinhibit

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Relugolix (Synonyms: TAK-385)

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