2. GPCR/G Protein
  3. TSH Receptor
  4. ML224

ML224  (Synonyms: NCGC00242364; ANTAG3)

Cat. No.: HY-12381 Purity: 99.18%
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ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.

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

ML224 Chemical Structure

ML224 Chemical Structure

CAS No. : 1338824-21-7

Size Price Stock Quantity
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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 173 In-stock
Solution
10 mM * 1 mL in DMSO USD 173 In-stock
Solid
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10 mg USD 240 In-stock
50 mg USD 750 In-stock
100 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

ML224 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ML224

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ML224 (NCGC00242364) is a selective TSHR antagonist with an IC50 value of 2.1 µM. ML224 can be used in the study of Graves' disease and other thyroid disorders.

IC50 & Target[1]

TSHR

2.1 μM (IC50)

LHR

＞30 μM (IC50)

FSHR

＞30 μM (IC50)

In Vitro

ML224 (0.001-100 μM; 20 min) exhibits half-maximal inhibitory doses of 2.1 μM for TSHR and greater than 30 μM for LH and FSH receptors in human embryonic kidney 293 cells[1].

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

ML224 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human embryonic kidney 293 cells (stably expressing TSHRs, LHRs, or FSHRs)
Concentration: 0.001-100 µM
Incubation Time: 20 min
Result: Showed the IC50 for stimulation by bovine TSH (1.8 nM) was 2.1 µM.
Showed inhibition of LH and FSH stimulation was less than 15% for LH (1 nM) and less than 30% for FSH (1 nM) at 30 µM.
In Vivo

ANTAG3 (2 mg/mice; i.p. via osmotic pump; single daily for 3 days) lowers serum FT4 levels and thyroidal mRNAs for TPO and NIS in mice continuously stimulated by TRH[1].

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

Animal Model: Female BALB/c mice (8 to 13-week-old; ~18.7 g)[1].
Dosage: 2 mg/mice
Administration: Intraperitoneal injection via osmotic pump; single daily for 3 days
Result: Lowered the levels of FT4 by 44%, and the levels of TPO and NIS mRNAs by 75% and 83%, respectively.
Molecular Weight

525.59

Formula

C31H31N3O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(NC1=CC(C)=C(OCC2=CC(C(N3CC4=CC=CO4)NC5=C(C=CC=C5)C3=O)=CC=C2OC)C(C)=C1)=O
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 (190.26 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 1.9026 mL 9.5131 mL 19.0262 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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)

g

Dosing volume
(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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9026 mL 9.5131 mL 19.0262 mL 47.5656 mL
5 mM 0.3805 mL 1.9026 mL 3.8052 mL 9.5131 mL
10 mM 0.1903 mL 0.9513 mL 1.9026 mL 4.7566 mL
15 mM 0.1268 mL 0.6342 mL 1.2684 mL 3.1710 mL
20 mM 0.0951 mL 0.4757 mL 0.9513 mL 2.3783 mL
25 mM 0.0761 mL 0.3805 mL 0.7610 mL 1.9026 mL
30 mM 0.0634 mL 0.3171 mL 0.6342 mL 1.5855 mL
40 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1891 mL
50 mM 0.0381 mL 0.1903 mL 0.3805 mL 0.9513 mL
60 mM 0.0317 mL 0.1586 mL 0.3171 mL 0.7928 mL
80 mM 0.0238 mL 0.1189 mL 0.2378 mL 0.5946 mL
100 mM 0.0190 mL 0.0951 mL 0.1903 mL 0.4757 mL
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ML224 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:

ML2241338824-21-7NCGC00242364 ANTAG3ML 224ML-224NCGC 00242364NCGC-00242364ANTAG3ANTAG 3ANTAG-3TSH ReceptorThyrotropin receptorThyroid-stimulating hormone ReceptorGraves' diseasethyroid disorders293 cellsTSHRsLHRsFSHRsInhibitorinhibitorinhibit

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