GnRH-R antagonist 1

Name: GnRH-R antagonist 1
Brand: TargetMol
SKU: T72492
Rating: 4.5 (1 reviews)

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Catalog No. T72492Cas No. 2826273-90-7

GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1].

GnRH-R antagonist 1

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Catalog No. T72492Cas No. 2826273-90-7

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$2,420	10-14 weeks	10-14 weeks
50 mg	$3,180	10-14 weeks	10-14 weeks
100 mg	$4,300	10-14 weeks	10-14 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1].
In vitro	GnRH-R antagonist 1 demonstrates a cell permeability that is 140 times greater than that of Relugolix, while also showing favorable stability in both human and mouse microsomes [1].
In vivo	GnRH-R antagonist 1 administered orally at a dosage of 30 mg/kg once daily for seven days exhibits a good safety profile [1]. At a single oral dose of 12 mg/kg, it demonstrates favorable pharmacokinetics and high oral bioavailability, evident from a 44.7% F% value [1]. Furthermore, this dosage effectively suppresses circulating testosterone levels in rats for over 24 hours [1].

Chemical Properties

Molecular Weight	721.65
Formula	C₃₁H₂₈F₅N₇O₆S
Cas No.	2826273-90-7
Smiles	CN(CCOC(F)(F)F)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc