TELOTRISTAT ETHYL (LX1606)

Alias: LX 1032; LX 1606; LX-1032; LX1606; LX1032; LX-1606; trade name: Xermelo
Cat No.:V3927 Purity: ≥98%
Telotristat ethyl (formerly LX-1032; LX-1606; LX-1032; LX-1606; trade name:Xermelo), the ethyl ester prodrug form ofTelotristat,is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor (IC50= 0.028 μM) with antiserotonergic and anti-diarrhea activity.
TELOTRISTAT ETHYL (LX1606) Chemical Structure CAS No.: 1033805-22-9
Product category: Tryptophan Hydroxylase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
2mg
5mg
10mg
25mg
50mg
100mg
250mg
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Other Forms of TELOTRISTAT ETHYL (LX1606):

  • Telotristat Etiprate (LX 1606 Hippurate)
  • Telotristat (LP-778902)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Telotristat ethyl (formerly LX-1032; LX-1606; LX-1032; LX-1606; trade name: Xermelo), the ethyl ester prodrug form of Telotristat, is an orally bioavailable tryptophan hydroxylase (TPH) inhibitor (IC50 = 0.028 μM) with antiserotonergic and anti-diarrhea activity. As of 2017, Telotristat ethyl has been approved to treat carcinoid syndrome diarrhea. Telotristat has activity in controlling diarrhea associated with carcinoid syndrome. Telotristat acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. Blocking peripheral serotonin synthesis by telotristat reduces severity of both chemical- and infection-induced intestinal inflammation.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Telotristat (formerly known as LP-778902) is the active metabolite of LX1606 (Telotristat etiprate) which is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential an in vivo IC50 of 0.028 μM and with antiserotonergic activity. Telotristat has activity in controlling diarrhea associated with carcinoid syndrome. Telotristat acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. Blocking peripheral serotonin synthesis by telotristat reduces severity of both chemical- and infection-induced intestinal inflammation.


Kinase Assay: Telotristat (formerly known as LP-778902) is the active metabolite of LX1606 (Telotristat etiprate) which is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential an in vivo IC50 of 0.028 μM and with antiserotonergic activity.


Cell Assay: BON CBA cells are grown in equal volume of DMEM and F12K with 5% bovine serum for 3-4 hours (20 K cell/well) and telotristat is added at a concentration range of 0.07 to 50 μM. The cells are incubated at 37°C overnight. 50 μM of the culture supernatant is then taken for 5HTP measurement. The supernatant is mixed with equal volume of 1M TCA, then filtered through glass fiber. The filtrate is loaded on reverse phase HPLC for 5HTP concentration measurement. The cell viability is measured by treating the remaining cells with Celltiter-Glo Luminescent Cell Viability Assay.

ln Vivo
The peripheral but not the brain of the mice is less serotonin-containing when telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd) is administered. Telotristat ethyl (200 mg/kg po, qd) significantly protects against TNBS-induced elevation in blood neutrophil counts in a rat model of inflammatory bowel disease. The mouse IBD model is protected by telotristat ethyl (200 mg/kg po, qd), as shown by histopathological evaluation[1]. In the jejunum, telotristat ethyl (15, 50, 150, and 300 mg/kg) depletes 5-HT, but not in the brain. However, neither the constitutive gastrointestinal motility in mice nor the depletion of enteric neuronal serotonin (5-HT) are caused by telotristat ethyl (200 mg/kg, po). The severity of colitis caused by trinitrobenzene sulfonic acid (TNBS) is lessened by telotristat ethyl (200 mg/kg)[2].
Animal Protocol
Dissolved in 15% cyclodextrin or 0.25% methylcellulose; 300 mg/kg; p.o.
Male C57BL/6 mice and male C57 albino mice.
References
[1]. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model.
[2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H26CLF3N6O3
Molecular Weight
574.99
CAS #
1033805-22-9
SMILES
O=C(OCC)[C@@H](N)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
Synonyms
LX 1032; LX 1606; LX-1032; LX1606; LX1032; LX-1606; trade name: Xermelo
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ≥ 100 mg/mL
Water:N/A
Ethanol:N/A
Solubility (In Vivo)
O=C(OCC)[C@@H](N)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
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7392 mL 8.6958 mL 17.3916 mL
5 mM 0.3478 mL 1.7392 mL 3.4783 mL
10 mM 0.1739 mL 0.8696 mL 1.7392 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • TELOTRISTAT ETHYL

    Peripheral tryptophan hydroxylase inhibitors deplete serotonin (5-HT) from the gut and blood but not from the brain.Gut.2014 Jun;63(6):928-37.
  • TELOTRISTAT ETHYL

    Peripheral tryptophan hydroxylase inhibitors do not deplete enteric neuronal serotonin (5-HT).Gut.2014 Jun;63(6):928-37.

  • TELOTRISTAT ETHYL

    Peripheral tryptophan hydroxylase inhibitors fail to affect measures of constitutive gastrointestinal (GI) motility.Gut.2014 Jun;63(6):928-37.
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