4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine
- Product Name
- 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine
- CAS No.
- 945976-76-1
- Chemical Name
- 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine
- Synonyms
- LX-1031 (LX1031;inhibit,Inhibitor,LX1031,LX 1031,LX-1031,Tryptophan Hydroxylase;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
- CBNumber
- CB42554349
- Molecular Formula
- C28H25F3N4O4
- Formula Weight
- 538.52
- 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 Property
- 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)
N-Bromosuccinimide Price
- Product number
- CS-0452
- Product name
- LX-1031
- Purity
- 99.58%
- Packaging
- 5mg
- Price
- $228
- Updated
- 2021/12/16
- Product number
- CCH0012935
- Product name
- (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
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $317.9
- Updated
- 2021/12/16
- Product number
- CS-0452
- Product name
- LX-1031
- Purity
- 99.58%
- Packaging
- 10mg
- Price
- $396
- Updated
- 2021/12/16
- Product number
- CS-0452
- Product name
- LX-1031
- Purity
- 99.58%
- Packaging
- 25mg
- Price
- $792
- Updated
- 2021/12/16
- Product number
- A3565
- Product name
- LX-1031
- Packaging
- 250mg
- Price
- $1131
- Updated
- 2021/12/16
4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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