| Identification | Back Directory | [Name]
4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine | [CAS]
945976-76-1 | [Synonyms]
LX-1031
(LX1031
4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine
L-Phenylalanine, 4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-
4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine USP/EP/BP
(S)-2-amino-3-(4-(2-amino-6-((R)-2,2,2-trifluoro-1-(3’-methoxybiphenyl-4-yl)ethoxy)pyrimidin-4-yl)phenyl)propanoic acid
(S)-2-aMino-3-(4-(2-aMino-6-((R)-2,2,2-trifluoro-1-(3'-Methoxy-[1,1'-biphenyl]-4-yl)ethoxy)pyriMidin-4-yl)phenyl)propanoic acid | [Molecular Formula]
C28H25F3N4O4 | [MOL File]
945976-76-1.mol | [Molecular Weight]
538.52 |
| Chemical Properties | Back Directory | [Boiling point ]
715.6±70.0 °C(Predicted) | [density ]
1.349 | [storage temp. ]
Store at -20°C | [solubility ]
≥26.93 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O | [form ]
solid | [pka]
2.04±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally. | [Biological Activity]
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. | [in vitro]
lx-1031 inhibits tph1 at its concentration of 10-8–10-7 mol l-1 range [1]. | [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 [2]. | [target]
TPH | [References]
[1] camilleri m. lx-1031, a tryptophan 5-hydroxylase inhibitor, and its potential in chronic diarrhea associated with increased serotonin. neurogastroenterol motil. 2011;23(3):193-200.
[2] brown pm, jackson ji, frazier ks, turner ca, shi zc, liu q. from mouse knockout to investigational drug: lx1031, a novel potential treatment for irritable bowel syndrome. am j gastroenterol 2007; 102: s961 (abstract).
[3] freiman j, jackson j, frazier ks, yang qm, liu q, brown p. lx1031: inhibition of 5-ht synthesis as a new target in the management of irritable bowel syndrome (ibs). neurogastroenterol motil 2009; 21: 250. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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