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

ML224  (Synonyms: NCGC00242364; ANTAG3)

Cat. No.: HY-12381 Purity: 99.71%
COA Handling Instructions

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

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Solution
10 mM * 1 mL in DMSO USD 173 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 173 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 240 In-stock
50 mg USD 750 In-stock
100 mg USD 1200 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

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].

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].

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

Appearance

Solid

Formula

C31H31N3O5
CAS No.
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)

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
10 mM 0.1903 mL 0.9513 mL 1.9026 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

  • Molarity Calculator

  • Dilution Calculator

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: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

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