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ML224

CAS No. 1338824-21-7

ML224( —— )

Catalog No. M33433 CAS No. 1338824-21-7

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    ML224
  • Note
    Research use only, not for human use.
  • Brief Description
    ML224 (NCGC00242364) is a TSHR antagonist for the treatment of Graves' orbital disease and Graves' hyperthyroidism.
  • 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.
  • In Vitro
    Cell Viability Assay 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
    Animal Model:Female BALB/c mice (8 to 13-week-old; ~18.7 g).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.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    TSH Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1338824-21-7
  • Formula Weight
    525.59
  • Molecular Formula
    C31H31N3O5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (190.26 mM; Ultrasonic )
  • SMILES
    COc1ccc(cc1COc1c(C)cc(NC(C)=O)cc1C)C1Nc2ccccc2C(=O)N1Cc1ccco1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Neumann S, et al. A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology. 2014 Jan;155(1):310-4.?
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