Home >> Research Area >>Metabolism>>TPH>> LX1606

LX1606

Tryptophan hydroxylase (TPH) inhibitor CAS# 1137608-69-5

LX1606

Catalog No. BCC1713----Order now to get a substantial discount!

Product Name & Size Price Stock
LX1606: 5mg $138 In Stock
LX1606: 10mg Please Inquire In Stock
LX1606: 20mg Please Inquire Please Inquire
LX1606: 50mg Please Inquire Please Inquire
LX1606: 100mg Please Inquire Please Inquire
LX1606: 200mg Please Inquire Please Inquire
LX1606: 500mg Please Inquire Please Inquire
LX1606: 1000mg Please Inquire Please Inquire
Related Products
  • Telotristat

    Catalog No.:BCC5128
    CAS No.:1033805-28-5
  • LX-1031

    Catalog No.:BCC1712
    CAS No.:945976-76-1

Quality Control of LX1606

Number of papers citing our products

Chemical structure

LX1606

3D structure

Chemical Properties of LX1606

Cas No. 1137608-69-5 SDF Download SDF
PubChem ID 25253377 Appearance Powder
Formula C36H35ClF3N7O6 M.Wt 754.17
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Telotristat etiprate
Solubility DMSO : ≥ 28 mg/mL (37.13 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-benzamidoacetic acid;ethyl (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoate
SMILES CCOC(=O)C(CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)OC(C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N.C1=CC=C(C=C1)C(=O)NCC(=O)O
Standard InChIKey XSFPZBUIBYMVEA-CELUQASASA-N
Standard InChI InChI=1S/C27H26ClF3N6O3.C9H9NO3/c1-3-39-25(38)20(32)12-16-4-6-17(7-5-16)21-14-23(35-26(33)34-21)40-24(27(29,30)31)19-9-8-18(28)13-22(19)37-11-10-15(2)36-37;11-8(12)6-10-9(13)7-4-2-1-3-5-7/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35);1-5H,6H2,(H,10,13)(H,11,12)/t20-,24+;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of LX1606

DescriptionLX1606 Hippurate is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.In Vivo:LX1606 (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. LX1606 (200 mg/kg po, qd) prevents the increase in blood neutrophil counts that is observed after TNBS challenge, provides significant protection in a mouse model of inflammatory bowel disease. LX1606 (200 mg/kg po, qd) protects the mouse IBD model confirmed by histopathology evaluation[1]. LX1606 (15, 50, 150, 300 mg/kg) depletes 5-HT from the jejunum but not the brain. But LX1606 (200 mg/kg, p.o.) does not deplete enteric neuronal serotonin (5-HT), or alter constitutive gastrointestinal motility in mice. LX1606 (200 mg/kg) alleviates the severity of trinitrobenzene sulfonic acid (TNBS)-induced colitis[2].

References:
[1]. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model. [2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013.

Protocol

Animal Administration [2]
For studies of the effects of peripheral TPH inhibitors on gut and brain 5-HT concentrations, LP-920540 is formulated in 0.1% Tween 80 in 0.25% methylcellulose and administered to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. LX1606 is formulated in 15% cyclodextrin (CaptisolTM, pH 3-4) or 0.25% methylcellulose and given to mice once daily via oral gavage at 10 mL/kg for 4 consecutive days. Whole brain, jejunum and colon (mesentery fat removed, gut lumen opened and blotted dry) are collected, snap frozen, and stored at -80ºC for future. LP-920540, LX1606, LP-778914, LP-778920 and vehicle control are also formulated with 0.5% methycellulose at appropriate doses in coded vials. The contents of the coded vials are given by oral gavage in amounts determined by the weights of the recipient mice. After the experiments, results are analyzed.

References:
[1]. Tamas Oravecz, et al. LX1606 (aka LX1032), a Novel Inhibitor of Serotonin Synthesis, Alleviates Development of Inflammatory Bowel Disease in a Preclinical Model. [2]. Margolis, K.G., et al., Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine. Gut, 2013.

LX1606 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

LX1606 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of LX1606

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.326 mL 6.6298 mL 13.2596 mL 26.5192 mL 33.149 mL
5 mM 0.2652 mL 1.326 mL 2.6519 mL 5.3038 mL 6.6298 mL
10 mM 0.1326 mL 0.663 mL 1.326 mL 2.6519 mL 3.3149 mL
50 mM 0.0265 mL 0.1326 mL 0.2652 mL 0.5304 mL 0.663 mL
100 mM 0.0133 mL 0.0663 mL 0.1326 mL 0.2652 mL 0.3315 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on LX1606

LX1606 (LX 1606, LX-1606) is an orally bioavailable, small-molecule, tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. LX1606 (LX 1606, LX-1606) is useful for Neurological Diseas.

Featured Products
New Products
 

References on LX1606

Blocking peripheral serotonin synthesis by telotristat etiprate (LX1032/LX1606) reduces severity of both chemical- and infection-induced intestinal inflammation.[Pubmed:26206858]

Am J Physiol Gastrointest Liver Physiol. 2015 Sep 15;309(6):G455-65.

Mucosal inflammation is accompanied by an alteration in 5-HT. Intestinal 5-HT synthesis is catalyzed by tryptophan hydroxylase 1 (Tph1) and we have shown that mice deficient in this rate-limiting enzyme have reduced severity of intestinal inflammation in models of chemical-induced experimental colitis. Here, we investigated the effect of blocking peripheral 5-HT synthesis in generation of intestinal inflammation by a using peripheral Tph inhibitor, telotristat etiprate (LX1606), in models of intestinal inflammation. LX1606 was given orally either prophylactically or therapeutically to mice with dextran sulfate sodium (DSS)-induced colitis or with infection with Trichuris muris. Severity of intestinal inflammation was measured by assessment of disease activity scores, histological damage, and MPO and inflammatory cytokine levels. LX1606 significantly reduced intestinal 5-HT levels and delayed onset and severity of DSS-induced acute and chronic colitis. This was associated with decreased MPO and proinflammatory cytokine levels compared with vehicle-treated controls. In the infection-induced inflammation model, treatment with LX1606 enhanced worm expulsion as well as increased IL-10 production and goblet cell numbers. LX1606-treated mice had significantly lower MPO and IL-1beta levels compared with controls postinfection. Our results demonstrate that peripheral 5-HT plays an important role in intestinal inflammation and in the generation of immune responses. Pharmacological reduction of peripheral 5-HT may serve as a potential strategy for modulating various intestinal inflammatory disorders.

Description

Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

Keywords:

LX1606,1137608-69-5,Telotristat etiprate,Natural Products,TPH, buy LX1606 , LX1606 supplier , purchase LX1606 , LX1606 cost , LX1606 manufacturer , order LX1606 , high purity LX1606

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: