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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Telotristat Etiprate (LX1606 etiprate; LX1032; LX-1032; LX-1606) is the hippurate salt of telotristat ethyl, which is a prodrug of Telotristat. Telotristat ethyl (trade name: Xermelo) is an orally bioavailable and peripheral tryptophan hydroxylase (TPH) inhibitor with potential antiserotonergic activity. Telotristat etiprate is converted under in vivo condition to the active form, telotristat (LP-778902), which binds to and inhibits the activity of TPH. Telotristat etiprate is useful in controlling diarrhea associated with carcinoid syndrome. Telotristat Etiprate acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels.
ln Vitro |
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ln Vivo |
Serotonin levels in the peripheral are decreased by telotristat ethyl (15, 50, 150, 300 mg/kg, po, qd), but not in the mouse brain. Telotristat ethyl (200 mg/kg po, qd) significantly protects mice against inflammatory bowel disease and inhibits the rise in blood neutrophil counts seen following TNBS challenge. Histopathological evaluation of a mouse model of IBD confirms that telotristat ethyl (200 mg/kg po, qd) protects the model [1]. In the jejunum, telotristat ethyl (15, 50, 150, and 300 mg/kg) depletes 5-HT, but not in the brain. Nevertheless, neither constitutive gastrointestinal motility nor serotonin (5-HT) depletion of enteric neurons occurs in mice treated with telotristat ethyl (200 mg/kg, po). The severity of colitis caused by trinitrobenzene sulfonic acid (TNBS) is lessened by telotristat ethyl (200 mg/kg) [2].
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Animal Protocol |
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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 |
Molecular Formula |
C27H26CLF3N6O3.C9H9NO3
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Molecular Weight |
754.15
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CAS # |
1137608-69-5
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Related CAS # |
Telotristat ethyl;1033805-22-9;Telotristat;1033805-28-5
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SMILES |
O=C(OCC)[C@@H](N)CC1=CC=C(C2=NC(N)=NC(O[ C@H](C3=CC=C(Cl)C=C3N4N=C(C)C=C4)C(F)(F)F)=C2)C=C1.O=C(O)CNC(C5=CC=CC=C5)=O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3260 mL | 6.6300 mL | 13.2600 mL | |
5 mM | 0.2652 mL | 1.3260 mL | 2.6520 mL | |
10 mM | 0.1326 mL | 0.6630 mL | 1.3260 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.