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Chemical Structure| 1137608-69-5 Chemical Structure| 1137608-69-5

Structure of Telotristat etiprate
CAS No.: 1137608-69-5

Chemical Structure| 1137608-69-5

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Telotristat etiprate (LX1606 Hippurate) is a tryptophan hydroxylase inhibitor that reduces serotonin production.

Synonyms: LX1606 Hippurate; LX 1032 hippurate

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Product Details of Telotristat etiprate

CAS No. :1137608-69-5
Formula : C36H35ClF3N7O6
M.W : 754.15
SMILES Code : O=C([C@H](CC1=CC=C(C=C1)C2=CC(O[C@H](C3=C(C=C(C=C3)Cl)N4C=CC(C)=N4)C(F)(F)F)=NC(N)=N2)N)OCC.O=C(C5=CC=CC=C5)NCC(O)=O
Synonyms :
LX1606 Hippurate; LX 1032 hippurate
MDL No. :MFCD22741520

Safety of Telotristat etiprate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Hydroxylase

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Mouse model of serotonin-secreting neuroendocrine neoplasm Oral 14 mg/kg/day Daily administration for 6 weeks To evaluate the effect of telotristat alone or in combination with octreotide on heart valve fibrosis. Results showed a clinically relevant, though non-significant, reduction in plasma NT-proBNP levels with telotristat alone and in combination with octreotide, but no significant effect on heart valve fibrosis. Int J Mol Sci. 2024 Feb 7;25(4):2036
Mice TNBS-induced colitis model Oral 200 mg/kg Daily administration for 5 days To evaluate the protective effect of LX1032 on TNBS-induced colitis. Results showed that LX1032 significantly reduced the severity of colitis, decreased the expression of inflammation-related genes, and reduced weight loss. Gut. 2014 Jun;63(6):928-37
Rats Wistar rats Oral 6, 20 and 60 mg/kg Single dose Evaluate the inhibitory effect of Telotristat on 5-HT synthesis Sci Rep. 2016 Jul 21;6:30059

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02026063 Carcinoid Syndrome PHASE3 COMPLETED 2018-09-12 Lexicon Investigational Site, ... More >>Mobile, Alabama, 36604, United States|Lexicon Investigational Site, Stanford, California, 94305, United States|Lexicon Investigational Site, Iowa City, Iowa, 52242, United States|Lexicon Investigational Site, Lexington, Kentucky, 40536, United States|Lexicon Investigational Site, Boston, Massachusetts, 02215, United States|Lexicon Investigational Site, New York, New York, 10029, United States|Lexicon Investigational Site, Philadelphia, Pennsylvania, 19104, United States|Lexicon Investigational Site, St. Leonards, New South Wales, 2065, Australia|Lexicon Investigational Site, Herston, Queensland, 4029, Australia|Lexicon Investigational Site, East Melbourne, Victoria, 3002, Australia|Lexicon Investigational Site, Edegem, B-2650, Belgium|Lexicon Investigational Site, Ghent, 9000, Belgium|Lexicon Investigational Site, Yvoir, 5530, Belgium|Lexicon Investgational Site, Calgary, Alberta, T2N4N2, Canada|Lexicon Investigational Site, Halifax, Nova Scotia, B0J1N0, Canada|Lexicon Investigational Site, Lille, 59037, France|Lexicon Investigational Site, Lyon, 69437, France|Lexicon Investigational Site, Villejuif, 94805, France|Lexicon Investigational Site, Bad Berka, 99437, Germany|Lexicon Investigational Site, Berlin, 13353, Germany|Lexicon Investigational Site, Essen, 45147, Germany|Lexicon Investigational Site, Hamburg, 20246, Germany|Lexicon Investigational Site, Marburg, 35043, Germany|Lexicon Investigational Site, Jerusalem, 91120, Israel|Lexicon Investigational Site, Milano, 20089, Italy|Lexicon Investigational Site, Milano, 20141, Italy|Lexicon Investigational Site, Pisa, 56124, Italy|Lexicon Investigational Site, Torino, 10043, Italy|Lexicon Investigational Site, Amsterdam, 1105AZ, Netherlands|Lexicon Investigational Site, Noord Holland, 1066CX, Netherlands|Lexicon Investigational Site, Noord-Brahant, 5631BM, Netherlands|Lexicon Investigational Site, Barcelona, 08035, Spain|Lexicon Investigational Site, Madrid, 28034, Spain|Lexicon Investigational Site, Seville, 41013, Spain|Lexicon Investigational Site, Lund, 22185, Sweden|Lexicon Investigational Site, Uppsala, 75185, Sweden|Lexicon Investigational Site, Coventry, CV22DX, United Kingdom|Lexicon Investigational Site, Glasgow, G120YN, United Kingdom|Lexicon Investigational Site, London, NW32QG, United Kingdom|Lexicon Investigational Site, London, SE59RS, United Kingdom|Lexicon Investigational Site, London, W120HS, United Kingdom|Lexicon Investigational Site, Manchester, M204BX, United Kingdom|Lexicon Investigational Site, Newcastle-Upon-Tyne, NE14LP, United Kingdom Less <<
NCT03442725 Renal Impairment PHASE1 COMPLETED 2018-05-13 A.T.C. s.a., Clinical Pharmaco... More >>logy Unit, CHU Sart-Tilman, Liège, B-4000, Belgium|CRS Clinical Research Services Kiel GmbH, Kiel, D-24105, Germany|ARENSIA Exploratory Medicine Phase I Unit, Republican Clinical Hospital, Chisinau, MD-2025, Moldova, Republic of|ARENSIA Unit in Spitalul de Nefrologie, Bucharest, Romania Less <<
NCT01104415 Carcinoid Syndrome PHASE2 COMPLETED 2014-02-12 Lexicon Investigational Site, ... More >>Bad Berka, Germany|Lexicon Investigational Site, Berlin, Germany|Lexicon Investigational Site, Halle, Germany|Lexicon Investigational Site, Lubeck, Germany|Lexicon Investigational Site, Marburg, Germany|Lexicon Investigational Site, Munich, Germany|Lexicon Investigational Site, Basingstoke, United Kingdom|Lexicon Investigational Site, Cambridge, United Kingdom|Lexicon Investigational Site, London, United Kingdom|Lexicon Investigational Site, Manchester, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.33mL

0.27mL

0.13mL

6.63mL

1.33mL

0.66mL

13.26mL

2.65mL

1.33mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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