1. Metabolic Enzyme/Protease
  2. Tryptophan Hydroxylase

LX1606 Hippurate (Synonyms: Telotristat etiprate; LX 1606 Hippurate; LX-1606 Hippurate)

Cat. No.: HY-13055
Handling Instructions

LX1606 Hippurate is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

For research use only. We do not sell to patients.
LX1606 Hippurate Chemical Structure

LX1606 Hippurate Chemical Structure

CAS No. : 1137608-69-5

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $199 In-stock
5 mg $130 In-stock
10 mg $240 In-stock
50 mg $800 In-stock
100 mg $1400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

LX1606 Hippurate is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

In Vivo

LX1606 (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. LX1606 (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. LX1606 (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation[1]. LX1606 (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But LX1606 (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. LX1606 (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02026063 Lexicon Pharmaceuticals Carcinoid Syndrome December 2013 Phase 3
NCT02063659 Lexicon Pharmaceuticals Carcinoid Syndrome March 11, 2014 Phase 3
NCT02157584 Lexicon Pharmaceuticals Healthy June 2014 Phase 1
NCT02147808 Lexicon Pharmaceuticals Drug Interactions May 2014 Phase 1
NCT01677910 Lexicon Pharmaceuticals Carcinoid Syndrome October 2012 Phase 3
NCT02157558 Lexicon Pharmaceuticals Drug Interactions July 2014 Phase 1
NCT02195635 Lexicon Pharmaceuticals Drug Interactions July 2014 Phase 1
NCT02155205 Lexicon Pharmaceuticals QT Interval May 2014 Phase 1
NCT02683577 Ipsen Hepatic Impairment February 2016 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Animal Administration
[2]

LX1606 is formulated in 15% cyclodextrin (CaptisolTM, pH 3-4) or 0.25% methylcellulose.

For studies of the effects of peripheral TPH inhibitors on gut and brain 5-HT concentrations, LP-920540 is formulated in 0.1% Tween 80 in 0.25% methylcellulose and administered to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. LX1606 is formulated in 15% cyclodextrin (CaptisolTM, pH 3-4) or 0.25% methylcellulose and given to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. Whole brain, jejunum and colon (mesentery fat removed, gut lumen opened and blotted dry) are collected, snap frozen, and stored at -80ºC for future. LP-920540, LX1606, LP-778914, LP-778920 and vehicle control are also formulated with 0.5% methycellulose at appropriate doses in coded vials. The contents of the coded vials are given by oral gavage in amounts determined by the weights of the recipient mice. After the experiments, results are analyzed.

References
M.Wt

754.15

Formula

C₃₆H₃₅ClF₃N₇O₆

CAS No.

1137608-69-5

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 28 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
LX1606 Hippurate
Cat. No.:
HY-13055
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