Telotristat Etiprate (LX 1606 Hippurate)

Catalog No.S2173

Telotristat Etiprate (LX 1606 Hippurate) Chemical Structure

Molecular Weight(MW): 754.15

Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.

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Biological Activity

Description Telotristat Etiprate (LX 1606 Hippurate) is an orally bioavailable, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Phase 3.
Targets
Tryptophan hydroxylase [1]
In vivo Telotristat Etiprate (300 mg/kg p.o.) significantly reduces 5-HT in the gut and blood, but not brain 5-HT. Telotristat Etiprate (200 mg/kg p.o.) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis with lower expression of some genes encoding inflammation-related cytokines and chemokines in mice. [2]

Protocol

Animal Research:

[2]

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  • Animal Models: Male C57BL/6 mice and male C57 albino mice.
  • Formulation: 15% cyclodextrin or 0.25% methylcellulose
  • Dosages: ~300 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (132.59 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 754.15
Formula

C27H26ClF3N6O3.C9H9NO3

CAS No. 1137608-69-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02683577 Completed Hepatic Impairment Ipsen February 2016 Phase 1
NCT02157558 Completed Drug Interactions Lexicon Pharmaceuticals July 2014 Phase 1
NCT02195635 Completed Drug Interactions Lexicon Pharmaceuticals July 2014 Phase 1
NCT02157584 Completed Healthy Lexicon Pharmaceuticals June 2014 Phase 1
NCT02147808 Completed Drug Interactions Lexicon Pharmaceuticals May 2014 Phase 1
NCT02155205 Completed QT Interval Lexicon Pharmaceuticals May 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Hydroxylase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID