Telotristat Etiprate (LX 1606 Hippurate)

Catalog No.S2173

For research use only.

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

Telotristat Etiprate (LX 1606 Hippurate) Chemical Structure

CAS No. 1137608-69-5

Selleck's Telotristat Etiprate (LX 1606 Hippurate) has been cited by 1 Publication

Purity & Quality Control

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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 (from reference)

Animal Research:

[2]

  • Animal Models: Male C57BL/6 mice and male C57 albino mice.
  • Dosages: ~300 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 754.15
Formula

C27H26ClF3N6O3.C9H9NO3

CAS No. 1137608-69-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC(=O)C(CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)OC(C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N.C1=CC=C(C=C1)C(=O)NCC(=O)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03442725 Completed Drug: Telotristat etiprate Renal Impairment Ipsen February 9 2018 Phase 1
NCT03423446 Completed Drug: Telotristat Ethyl Hepatic Impairment Lexicon Pharmaceuticals November 28 2017 Phase 1
NCT02683577 Completed Drug: telotristat etiprate Hepatic Impairment Ipsen February 2016 Phase 1
NCT02195635 Completed Drug: Telotristat etiprate|Drug: Octreotide acetate Drug Interactions Lexicon Pharmaceuticals July 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-11-29)

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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