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LX-1031

Names

[ CAS No. ]:
945976-76-1

[ Name ]:
LX-1031

[Synonym ]:
unii-j08e1j78gk
4-{2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy-4-biphenylyl)ethoxy]-4-pyrimidinyl}-L-phenylalanine
cs-0452
lx-1031
lx-1031||lx 1031
L-Phenylalanine, 4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-

Biological Activity

[Description]:

LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.

[Related Catalog]:

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

[In Vivo]

With oral administration of LX-1031 in mice, the average 5-HT reductions in the jejunum relative to control are appr 33, 51, and 66% with the 15, 45 and 135 mg/kg/day doses respectively. In a preliminary report, the effects of LX-1031, 100 mg/kg daily, on 5-HT levels in jejunal mucosa are reversible within 2 days of discontinuation in mice[1]. LX-1031 dose-dependently reduces expression of 5-HT in the duodenum, jejunum and ileum, but has no effect on brain 5-HT levels in preclinical assay[2].

[References]

[1]. Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor, and its potential in chronic diarrhea associated with increased serotonin. Neurogastroenterol Motil. 2011 Mar;23(3):193-200.

[2]. Camilleri M. LX-1031, a tryptophan 5-hydroxylase inhibitor that reduces 5-HT levels for the potential treatment of irritable bowel syndrome. IDrugs. 2010 Dec;13(12):921-8.


[Related Small Molecules]

Telotristat | DL-4-Chlorophenylalanine | LP-533401

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
715.6±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H25F3N4O4

[ Molecular Weight ]:
538.518

[ Flash Point ]:
386.6±35.7 °C

[ Exact Mass ]:
538.182800

[ PSA ]:
134.31000

[ LogP ]:
5.36

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.608

[ Storage condition ]:
2-8℃

Related Compounds