LX1606Tryptophan hydroxylase (TPH) inhibitor CAS# 1137608-69-5 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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. | ||
| Description | LX1606 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: | |||||
LX1606 Dilution Calculator
LX1606 Molarity Calculator
| 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. | |||||
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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.
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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.
