[CAS NO. 1033805-22-9] Telotristatethyl

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PRODUCTS SPECIFICATIONS [1033805-22-9]

Catalog

HY-13055A

Brand

MCE

CAS

1033805-22-9

DESCRIPTION [1033805-22-9]

Overview

MDL	-
Molecular Weight	574.98
Molecular Formula	C27H26ClF3N6O3
SMILES	N[C@@H](CC1=CC=C(C2=NC(N)=NC(O[C@H](C3=CC=C(Cl)C=C3N4N=C(C)C=C4)C(F)(F)F)=C2)C=C1)C(OCC)=O

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Nutrients. 2022, 14(1), 117.

Summary

Telotristat ethyl (LX1032) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

In Vivo

Telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. Telotristat ethyl (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation ^[1] . Telotristat ethyl (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But Telotristat ethyl (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. Telotristat ethyl (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03910387	Emory University\|TerSera Therapeutics LLC	Locally Advanced Unresectable Pancreatic Adenocarcinoma\|Metastatic Pancreatic Adenocarcinoma\|Recurrent Pancreatic Adenocarcinoma\|Stage III Pancreatic Cancer AJCC v8\|Stage IV Pancreatic Cancer AJCC v8	April 17, 2019	Phase 2
NCT04776876	M.D. Anderson Cancer Center	Advanced Neuroendocrine Neoplasm\|Carcinoid Syndrome	March 1, 2021	Phase 2
NCT01104415	Lexicon Pharmaceuticals	Carcinoid Syndrome	June 15, 2010	Phase 2
NCT02683577	Ipsen	Hepatic Impairment	February 2016	Phase 1
NCT00853047	Lexicon Pharmaceuticals	Carcinoid Syndrome	March 2009	Phase 2
NCT04065165	European Organisation for Research and Treatment of Cancer - EORTC\|Ipsen	Small Intestinal NET\|Carcinoid Heart Disease	April 2020	Phase 3
NCT03453489	Barbara Ann Karmanos Cancer Institute\|National Cancer Institute (NCI)	Carcinoid Syndrome\|Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm	June 20, 2018	Phase 2
NCT03423446	Lexicon Pharmaceuticals	Hepatic Impairment	November 28, 2017	Phase 1
NCT02157584	Lexicon Pharmaceuticals	Healthy	June 2014	Phase 1
NCT04810091	M.D. Anderson Cancer Center\|TerSera Therapeutics LLC	Locally Advanced Neuroendocrine Neoplasm\|Metastatic Neuroendocrine Neoplasm	May 18, 2021	Phase 3
NCT02195635	Lexicon Pharmaceuticals	Drug Interactions	July 2014	Phase 1
NCT04034745	Andrew Hendifar, MD\|Lexicon Pharmaceuticals\|Cedars-Sinai Medical Center	Pancreatic Cancer\|Neuroendocrine Tumors\|Cachexia; Cancer	October 2020
NCT04713202	Chandrikha Chandrasekhara\|TerSera Therapeutics LLC\|Big Ten Cancer Research Consortium	Neuroendocrine Tumors\|Carcinoid Syndrome\|Diarrhea	March 3, 2021	Phase 2
NCT02147808	Lexicon Pharmaceuticals	Drug Interactions	May 2014	Phase 1
NCT04672876	University of Chicago	Neuroendocrine Tumors	January 2022	Phase 2
NCT03442725	Ipsen	Renal Impairment	February 9, 2018	Phase 1
NCT01677910	Lexicon Pharmaceuticals	Carcinoid Syndrome	January 8, 2013	Phase 3
NCT02155205	Lexicon Pharmaceuticals	QT Interval	May 2014	Phase 1
NCT03302845	Lexicon Pharmaceuticals	Drug-drug Interaction	September 21, 2017	Phase 1
NCT01456052	Lexicon Pharmaceuticals	Ulcerative Colitis	January 30, 2012	Phase 2
NCT03790111	TerSera Therapeutics LLC	Biliary Tract Cancer	March 13, 2019	Phase 2
NCT02063659	Lexicon Pharmaceuticals	Carcinoid Syndrome	March 11, 2014	Phase 3
NCT02026063	Lexicon Pharmaceuticals	Carcinoid Syndrome	January 14, 2014	Phase 3
NCT02157558	Lexicon Pharmaceuticals	Drug Interactions	July 2014	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 101.5 mg/mL ( 176.53 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7392 mL	8.6960 mL	17.3919 mL
5 mM	0.3478 mL	1.7392 mL	3.4784 mL
10 mM	0.1739 mL	0.8696 mL	1.7392 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.35 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

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

4-[2-Amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]-4-pyrimidinyl]-L-phenylalanine ethyl ester

Telotristat ethyl

LX 1606

(2S)-2-Amino-3-[4-[2-amino-6-[[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethyl]oxy]pyrimidin-4-yl]phenyl]propionic acid ethyl ester

LX 1032

Xermelo