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LX-1031
Cat No.
CEI-1403
Description
LX-1031 is an oral, small molecule inhibitor of tryptophan 5-hydroxylase (TPH).
Product Overview
Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. Serotonin plays important physiological roles both peripherally and centrally. LX-1031 is a heterocyclic substituted phenylalanine analog, an oral small molecule tryptophan hydroxylase (TPH) inhibitor that reduces synthesis of serotonin (5-HT) peripherally and is being developed for conditions characterized by excess 5-HT expression such as diarrhea-predominant irritable bowel syndrome (IBS-D) and, possibly, carcinoid diarrhea. Clinical trial: In double-blind studies (doses of LX-1031 ranging from 250 to 1000 mg q. i. d.), average 5HIAA reductions of 33% were noted. In phase I studies, 54 healthy volunteers received the drug for up to 14 days while the diet was strictly controlled to avoid 5-HT-rich foods. Twenty four hour urine collections were obtained. Significant reductions in urinary 5-HIAA persisted over the duration of exposure.
CAS No.
945976-76-1
Molecular Weight
538.52
Purity
0.9852
Storage
Store at -20°C
Synonyms
LX1031; LX 1031
Targets
TPH
Molecular Formula
C28H25F3N4O4
Chemical Name
(2S)-2-amino-3-[4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-[4-(3-methoxyphenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
LX-1031 inhibits TPH1 at its concentration of 10-8-10-7 mol L-1 range.
In vivo
With oral administration of LX-1031 in mice, the 5-HT reductions in the jejunum relative to control were ~33%, 51%, and 66% with the 15, 45 and 135 mg/kg/day doses, respectively; the effect of 5 mg/kg/day on GI 5-HT content was not significantly different from control.
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