A TPH1 inhibitor
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Pro-drug Form(s)
25342Telotristat Etiprate
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Telotristat

Item No. 29424

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
CAS Number
1033805-28-5
Synonyms
  • LP778902
Molecular Formula
C25H22ClF3N6O3
Formula Weight
546.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:3): 0.25 mg/mlEthanol: 0.5 mg/ml
λmax
246, 307 nm
SMILES
NC1=NC(C2=CC=C(C[C@H](N)C(O)=O)C=C2)=CC(O[C@H](C3=CC=C(Cl)C=C3N4C=CC(C)=N4)C(F)(F)F)=N1
InChi Code
InChI=1S/C25H22ClF3N6O3/c1-13-8-9-35(34-13)20-11-16(26)6-7-17(20)22(25(27,28)29)38-21-12-19(32-24(31)33-21)15-4-2-14(3-5-15)10-18(30)23(36)37/h2-9,11-12,18,22H,10,30H2,1H3,(H,36,37)(H2,31,32,33)/t18-,22+/m0/s1
InChi Key
NCLGDOBQAWBXRA-PGRDOPGGSA-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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    Product Description

    Telotristat is a tryptophan hydroxylase 1 (TPH1) inhibitor (IC50 = 16 nM).1 Dietary administration of telotristat to pregnant and lactating mice decreases serotonin (5-HT; Item No. 14332) levels in maternal serum and decreases the femoral bone volume to tissue volume ratio, trabecular number and thickness, and cortical tissue mineral density, as well as serum calcium levels, in pups.2

    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. Weaver, S.R., Fricke, H.P., Xie, C., et al. Peripartum dietary supplementation of a small-molecule inhibitor of tryptophan hydroxylase 1 compromises infant, but not maternal, bone. Am. J. Physiol. Endocrinol. Metab. 215(6), E1133-E1142 (2018).