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LX-1031

Catalog No.GC15998

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LX-1031 Chemical Structure

Cas No.: 945976-76-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$203.00
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2mg
$99.00
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5mg
$171.00
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10mg
$297.00
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25mg
$594.00
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50mg
$990.00
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100mg
$1,665.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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].

Clinical trial: In double-blind studies (doses of LX-1031 ranging from 250 to 1000 mg q.i.d.), average 5HIAA reductions of 33% were noted. In phase I studies, 54 healthy volunteers received the drug for up to 14 days while the diet was strictly controlled to avoid 5-HT-rich foods. Twenty four hour urine collections were obtained. Significant reductions in urinary 5-HIAA persisted over the duration of exposure [3].

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.

Chemical Properties

Cas No. 945976-76-1 SDF
Chemical Name (2S)-2-amino-3-[4-[2-amino-6-[(1R)-2,2,2-trifluoro-1-[4-(3-methoxyphenyl)phenyl]ethoxy]pyrimidin-4-yl]phenyl]propanoic acid
Canonical SMILES COC1=CC=CC(=C1)C2=CC=C(C=C2)C(C(F)(F)F)OC3=NC(=NC(=C3)C4=CC=C(C=C4)CC(C(=O)O)N)N
Formula C28H25F3N4O4 M.Wt 538.52
Solubility ≥ 26.9 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.8569 mL 9.2847 mL 18.5694 mL
5 mM 0.3714 mL 1.8569 mL 3.7139 mL
10 mM 0.1857 mL 0.9285 mL 1.8569 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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