A prodrug form of telotristat
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Active Metabolite(s)
29424Telotristat
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Telotristat Etiprate

Item No. 25342

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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, compd. with N-benzoylglycine
CAS Number
1137608-69-5
Synonyms
  • LX 1032 hippurate
  • LX 1606 hippurate
Molecular Formula
C27H26ClF3N6O3 • C9H9NO3
Formula Weight
754.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 50 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.33 mg/mlEthanol: 5 mg/ml
λmax
242, 308 nm
SMILES
NC1=NC(O[C@@H](C(F)(F)F)C2=CC=C(Cl)C=C2N3N=C(C)C=C3)=CC(C4=CC=C(C[C@H](N)C(OCC)=O)C=C4)=N1.O=C(NCC(O)=O)C5=CC=CC=C5
InChi Code
InChI=1S/C27H26ClF3N6O3.C9H9NO3/c1-3-39-25(38)20(32)12-16-4-6-17(7-5-16)21-14-23(35-26(33)34-21)40-24(27(29,30)31)19-9-8-18(28)13-22(19)37-11-10-15(2)36-37;11-8(12)6-10-9(13)7-4-2-1-3-5-7/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35);1-5H,6H2,(H,10,13)(H,11,12)/t20-,24?;/m0./s1
InChi Key
XSFPZBUIBYMVEA-BAHZNLOQSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Cayman Chemical
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    Product Description

    Telotristat etiprate is a prodrug form of telotristat, which is an inhibitor of tryptophan hydroxylase 1 (TPH1).1 Telotristat etiprate (15-300 mg/kg) reduces levels of serotonin (5-HT; Item No. 14332) in mouse jejunum and blood but not brain.2 It inhibits increases in IL-1β and IL-6 levels, histological damage in the colon, and weight loss in a mouse model of trinitrobenzene sulfonic acid-induced colitis when administered at a dose of 200 mg/kg. In mice infected with the nematode T. muris, telotristat etiprate (300 mg/kg per day) reduces colonic levels of myeloperoxidase (MPO), IL-1β, and IL-17, as well as worm burden.3 Formulations containing telotristat etiprate have been used in the treatment of diarrhea associated with carcinoid syndrome.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Goldberg, D.R., De Lombaert, S., Aiello, R., et al. Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors. Bioorg. Med. Chem. Lett. 26(12), 2855-2860 (2016).

    2. Margolis, K.G., Sevanovic, K., Li, Z., et al. Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut 63(6), 928-937 (2014).

    3. Kim, J.J., Wang, H., Terc, J.D., et al. Blocking peripheral serotonin synthesis by telotristat etiprate (LX1032/LX1606) reduces severity of both chemical- and infection-induced intestinal inflammation. Am. J. Physiol Gastrointest. Liver Physiol. 309(6), G455-G465 (2015).