1. Metabolic Enzyme/Protease
  2. Tryptophan Hydroxylase
  3. Telotristat etiprate

Telotristat etiprate (Synonyms: LX1606 Hippurate)

Cat. No.: HY-13055 Purity: 99.77%
Handling Instructions

Telotristat etiprate (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.

Telotristat etiprate Chemical Structure

Telotristat etiprate Chemical Structure

CAS No. : 1137608-69-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 91 In-stock
Estimated Time of Arrival: December 31
5 mg USD 70 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 235 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

Clinical Trial
Molecular Weight

754.15

Formula

C₃₆H₃₅ClF₃N₇O₆

CAS No.

1137608-69-5

SMILES

O=C([[email protected]](CC1=CC=C(C=C1)C2=CC(O[[email protected]](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

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 : ≥ 28 mg/mL (37.13 mM)

*"≥" means soluble, but saturation unknown.

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.
References
Animal Administration
[2]

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. Telotristat ethyl 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, Telotristat ethyl, 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.

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

References

Purity: 99.77%

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Keywords:

Telotristat etiprateLX1606LX 1606LX-1606Tryptophan HydroxylaseInhibitorinhibitorinhibit

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Telotristat etiprate
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