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Telotristat

CAS No. 1033805-28-5

Telotristat( LP778902 | LP 778902 | LP-778902 )

Catalog No. M10166 CAS No. 1033805-28-5

Telotristat (LP-778902) is a potent, small-molecule inhibitor of peripheral serotonin synthesis, acts by inhibiting tryptophan hydroxylase (TPH) with IC50 of 28 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Telotristat
  • Note
    Research use only, not for human use.
  • Brief Description
    Telotristat (LP-778902) is a potent, small-molecule inhibitor of peripheral serotonin synthesis, acts by inhibiting tryptophan hydroxylase (TPH) with IC50 of 28 nM.
  • Description
    Telotristat (LP-778902) is a potent, small-molecule inhibitor of peripheral serotonin synthesis, acts by inhibiting tryptophan hydroxylase (TPH) with IC50 of 28 nM, demonstrates potential for the treatment of carcinoid syndrome.Gastric Cancer Approved.
  • In Vitro
    Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome.
  • In Vivo
    Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional.
  • Synonyms
    LP778902 | LP 778902 | LP-778902
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    TPH
  • Recptor
    TPH
  • Research Area
    Cancer
  • Indication
    Gastric Cancer

Chemical Information

  • CAS Number
    1033805-28-5
  • Formula Weight
    546.9288
  • Molecular Formula
    C25H22ClF3N6O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC1=NN(C=C1)C2=C(C=CC(=C2)Cl)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N
  • Chemical Name
    L-Phenylalanine, 4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]-4-pyrimidinyl]-

Shipping & Storage Information

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

Reference

1. Margolis KG, et al. Gut. 2014 Jun;63(6):928-37. 2. Kulke MH, et al. Endocr Relat Cancer. 2014 Oct;21(5):705-14. 3. Kulke MH, et al. J Clin Oncol. 2017 Jan;35(1):14-23. 4. Kim JJ, et al. Am J Physiol Gastrointest Liver Physiol.
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  • Telotristat etiprate

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