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ML224

ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

Catalog No. T16106Cas No. 1338824-21-7

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Purity:99.14%

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ML224

Catalog No. T16106Cas No. 1338824-21-7

ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Pack Size	Price	Availability
1 mg	$52	In Stock
5 mg	$123	In Stock
10 mg	$197	In Stock
25 mg	$383	In Stock
1 mL x 10 mM (in DMSO)	$142	In Stock

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Product Introduction

Bioactivity

Description	ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.
Targets&IC50	FSHR:＞30 μM, TSHR:2.1 μM, LHR:＞30 μM, HEK293 cells:2.1 μM
In vitro	In human embryonic kidney 293 cells, ML224 exhibits a half-maximal inhibitory concentration (IC50) of 2.1 μM against TSHR after a 20-minute exposure, with a range of 0.001-100 μM. The half-maximal inhibitory concentrations against LH and FSH receptors exceed 30 μM[1].
In vivo	ML224(ANTAG3) 2 mg per mouse; administered through intraperitoneal infusion pump; once daily for 3 days) reduces serum FT4 levels and thyroid mRNA of TPO and NIS in mice subjected to prolonged TRH stimulation[1].
Alias	NCGC00242364, ANTAG3

Chemical Properties

Molecular Weight	525.59
Formula	C₃₁H₃₁N₃O₅
Cas No.	1338824-21-7

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 80 mg/mL (152.21 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9026 mL	9.5131 mL	19.0262 mL	95.1312 mL
5 mM	0.3805 mL	1.9026 mL	3.8052 mL	19.0262 mL
10 mM	0.1903 mL	0.9513 mL	1.9026 mL	9.5131 mL
20 mM	0.0951 mL	0.4757 mL	0.9513 mL	4.7566 mL
50 mM	0.0381 mL	0.1903 mL	0.3805 mL	1.9026 mL
100 mM	0.0190 mL	0.0951 mL	0.1903 mL	0.9513 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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