Home Metabolism Hydroxylase inhibitor Telotristat Etiprate (LX 1606 Hippurate) For research use only.

Telotristat Etiprate (LX 1606 Hippurate)

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

Telotristat Etiprate (LX 1606 Hippurate) Chemical Structure

CAS: 1137608-69-5

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

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Signaling Pathway

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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
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]
Animal Research Animal Models Male C57BL/6 mice and male C57 albino mice.
Dosages ~300 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03442725 Completed
Renal Impairment
Ipsen
 February 9 2018 Phase 1
NCT03423446 Completed
Hepatic Impairment
Lexicon Pharmaceuticals
 November 28 2017 Phase 1
NCT02683577 Completed
Hepatic Impairment
Ipsen
 February 2016 Phase 1
NCT02195635 Completed
Drug Interactions
Lexicon Pharmaceuticals
 July 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 754.15 Formula

C27H26ClF3N6O3.C9H9NO3
CAS No. 1137608-69-5 SDF Download Telotristat Etiprate (LX 1606 Hippurate) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (132.59 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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