ChemicalBook > CAS DataBase List > 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine

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;(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
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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 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)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0452
Product name
LX-1031
Purity
99.58%
Packaging
5mg
Price
$228
Updated
2021/12/16
American Custom Chemicals Corporation
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
ChemScene
Product number
CS-0452
Product name
LX-1031
Purity
99.58%
Packaging
10mg
Price
$396
Updated
2021/12/16
ChemScene
Product number
CS-0452
Product name
LX-1031
Purity
99.58%
Packaging
25mg
Price
$792
Updated
2021/12/16
ApexBio Technology
Product number
A3565
Product name
LX-1031
Packaging
250mg
Price
$1131
Updated
2021/12/16
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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 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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4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanine Suppliers

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945976-76-1, 4-[2-Amino-6-[(1R)-2,2,2-trifluoro-1-(3'-methoxy[1,1'-biphenyl]-4-yl)ethoxy]-4-pyrimidinyl]-L-phenylalanineRelated Search:


  • 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
  • (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
  • 945976-76-1