[CAS NO. 1137608-69-5] Telotristatetiprate

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PRODUCTS SPECIFICATIONS [1137608-69-5]

Catalog

HY-13055

Brand

MCE

CAS

1137608-69-5

DESCRIPTION [1137608-69-5]

Overview

MDL	MFCD22741520
Molecular Weight	754.15
Molecular Formula	C36H35ClF3N7O6
SMILES	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

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

1 Publications Citing Use of MCE

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

Summary

Telotristat etiprate (LX1606 Hippurate) 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
NCT04034745	Andrew Hendifar, MD\|Lexicon Pharmaceuticals\|Cedars-Sinai Medical Center	Pancreatic Cancer\|Neuroendocrine Tumors\|Cachexia; Cancer	October 2020
NCT03423446	Lexicon Pharmaceuticals	Hepatic Impairment	November 28, 2017	Phase 1
NCT02063659	Lexicon Pharmaceuticals	Carcinoid Syndrome	March 11, 2014	Phase 3
NCT02155205	Lexicon Pharmaceuticals	QT Interval	May 2014	Phase 1
NCT02157584	Lexicon Pharmaceuticals	Healthy	June 2014	Phase 1
NCT03442725	Ipsen	Renal Impairment	February 9, 2018	Phase 1
NCT01104415	Lexicon Pharmaceuticals	Carcinoid Syndrome	June 15, 2010	Phase 2
NCT00853047	Lexicon Pharmaceuticals	Carcinoid Syndrome	March 2009	Phase 2
NCT04672876	University of Chicago	Neuroendocrine Tumors	January 2022	Phase 2
NCT04810091	M.D. Anderson Cancer Center\|TerSera Therapeutics LLC	Locally Advanced Neuroendocrine Neoplasm\|Metastatic Neuroendocrine Neoplasm	May 18, 2021	Phase 3
NCT03790111	TerSera Therapeutics LLC	Biliary Tract Cancer	March 13, 2019	Phase 2
NCT02157558	Lexicon Pharmaceuticals	Drug Interactions	July 2014	Phase 1
NCT04713202	Chandrikha Chandrasekhara\|TerSera Therapeutics LLC\|Big Ten Cancer Research Consortium	Neuroendocrine Tumors\|Carcinoid Syndrome\|Diarrhea	March 3, 2021	Phase 2
NCT04776876	M.D. Anderson Cancer Center	Advanced Neuroendocrine Neoplasm\|Carcinoid Syndrome	March 1, 2021	Phase 2
NCT02026063	Lexicon Pharmaceuticals	Carcinoid Syndrome	January 14, 2014	Phase 3
NCT01456052	Lexicon Pharmaceuticals	Ulcerative Colitis	January 30, 2012	Phase 2
NCT04065165	European Organisation for Research and Treatment of Cancer - EORTC\|Ipsen	Small Intestinal NET\|Carcinoid Heart Disease	April 2020	Phase 3
NCT03302845	Lexicon Pharmaceuticals	Drug-drug Interaction	September 21, 2017	Phase 1
NCT03453489	Barbara Ann Karmanos Cancer Institute\|National Cancer Institute (NCI)	Carcinoid Syndrome\|Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm	June 20, 2018	Phase 2
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
NCT01677910	Lexicon Pharmaceuticals	Carcinoid Syndrome	January 8, 2013	Phase 3
NCT02195635	Lexicon Pharmaceuticals	Drug Interactions	July 2014	Phase 1
NCT02147808	Lexicon Pharmaceuticals	Drug Interactions	May 2014	Phase 1
NCT02683577	Ipsen	Hepatic Impairment	February 2016	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL ( 265.20 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3260 mL	6.6300 mL	13.2600 mL
5 mM	0.2652 mL	1.3260 mL	2.6520 mL
10 mM	0.1326 mL	0.6630 mL	1.3260 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: ≥ 10 mg/mL (13.26 mM); Clear solution
2.

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

Solubility: ≥ 10 mg/mL (13.26 mM); Clear solution

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