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LX1606

Names

[ CAS No. ]:
1137608-69-5

[ Name ]:
LX1606

[Synonym ]:
L-Phenylalanine, 4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]-4-pyrimidinyl]-, ethyl ester, compd. with glycine, N-benzoyl- (1:1)
(S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate hippurate
N-Benzoylglycine - ethyl 4-(2-amino-6-{(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy}-4-pyrimidinyl)-L-phenylalaninate (1:1)
Telotristat Etiprate
Telotristat etiprate (USAN)
LX1606
LX1032 hippurate
LX1606 Hippurate

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Tryptophan Hydroxylase
Research Areas >> Neurological Disease

[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].

[Animal admin]

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.

[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.


[Related Small Molecules]

Telotristat | DL-4-Chlorophenylalanine | LX-1031 | LP-533401

Chemical & Physical Properties

[ Melting Point ]:
145 °C

[ Molecular Formula ]:
C36H35ClF3N7O6

[ Molecular Weight ]:
754.155

[ Exact Mass ]:
753.228943

[ PSA ]:
197.57000

[ LogP ]:
7.16200

[ Storage condition ]:
-20℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds