Telotristat Etiprate (LX 1606 Hippurate)

Catalog No.S2173

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

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Telotristat Etiprate (LX 1606 Hippurate) Chemical Structure

Telotristat Etiprate (LX 1606 Hippurate) Chemical Structure
Molecular Weight: 754.15

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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 vitro
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]
Features

Protocol(Only for Reference)

Animal Study:

[2]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Pappas C, et al. J Clin Oncol 27, 2009 (suppl; abstr e14555).

[2] Margolis KG, et al. Gut. 2014, 63(6), 928-937.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-18)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02683577 Recruiting Hepatic Impairment Ipsen February 2016 Phase 1
NCT02195635 Active, not recruiting Drug Interactions Lexicon Pharmaceuticals July 2014 Phase 1
NCT02157558 Completed Drug Interactions Lexicon Pharmaceuticals July 2014 Phase 1
NCT02157584 Completed Healthy Lexicon Pharmaceuticals June 2014 Phase 1
NCT02155205 Completed QT Interval Lexicon Pharmaceuticals May 2014 Phase 1

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Chemical Information

Download Telotristat Etiprate (LX 1606 Hippurate) SDF
Molecular Weight (MW) 754.15
Formula

C27H26ClF3N6O3.C9H9NO3

CAS No. 11137608-69-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (132.59 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or 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 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]-, ethyl ester, compd. with N-benzoylglycine (1:1)

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.

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