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Telotristat CAS: 1033805-28-5

Category: Inhibitors
Product Name: Telotristat
Cat No: I000203
CAS No: 1033805-28-5
Synonyms: (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoic acid
Molecular Formula: C25H22ClF3N6O3
Molecular Weight: 546.93
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
Solubility: 10 mM in DMSO
Target: TPH
Storage: Store at RT
CAS 1033805-28-5,Telotristat
  • Description

Telotristat is the active metabolite of LX1606(Telotristat etiprate), which is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity.
IC50 value:
Target: tryptophan hydroxylase
in vitro:
in vivo: LX1606 (LX 1606, LX-1606) is useful for Neurological Diseas [1]. LX1606 were given orally to mice. LX1606 reduced 5-HT significantly in the gut and blood but not in the brain. oral LX1032 reduced the severity of TNBS-induced colitis; the expression of 24% of 84 genes encoding inflammation-related cytokines and chemokines was lowered at least fourfold and the reduced expression of 17% was statistically significant [1]. Treatment with LX1606 showed a strong positive effect in ameliorating TNBS-induced IBD in mice as assessed by various parameters of disease development. These preclinical data demonstrate that inhibition of TPH activity by LX1606 may provide a new approach for the treatment of IBD and its serotonin-mediated symptoms[3].

  • References

[1]. http://www.cancer.gov/drugdictionary/?CdrID=662188
[2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013.
[3]. ttp://assets.cureus.com/uploads/poster/file/46/d.pdf

price inquiry for CAS:1033805-28-5, Product:Telotristat