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| | 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Basic information |
| Product Name: | 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine | | Synonyms: | 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine;(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;(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;LX-1031
(LX1031;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;inhibit,Inhibitor,LX1031,LX 1031,LX-1031,Tryptophan Hydroxylase | | CAS: | 945976-76-1 | | MF: | C28H25F3N4O4 | | MW: | 538.52 | | EINECS: | | | Product Categories: | | | Mol File: | 945976-76-1.mol | ![4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Structure](CAS/20180906/GIF/945976-76-1.gif) |
| | 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Chemical Properties |
| 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 | | pka | 2.04±0.10(Predicted) | | form | solid |
| | 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Usage And Synthesis |
| 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. |
| | 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Preparation Products And Raw materials |
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