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Telotristat ethyl

Cat. No. M8913
Telotristat ethyl Structure
Synonym:

LX1606

Size Price Availability
10mg USD 320 4-7 Days
50mg USD 1100 4-7 Days
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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

LX1606 (15, 50, 150, 300 mg/kg, po, qd) reduces serotonin content in the periphery, but not in the brain of the mice. Telotristat ethyl (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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models mice
Formulation formulated in 15% cyclodextrin (Captisol, pH 3-4) or 0.25% methylcellulose
Dosages 10 mL/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 574.98
Formula C27H26ClF3N6O3
CAS Number 1033805-22-9
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Pharmacological reduction of mucosal but not neuronal serotonin opposes inflammation in mouse intestine.
Margolis KG, et al. Gut. 2014 Jun;63(6):928-37. PMID: 23749550.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Telotristat ethyl, LX1606 supplier, inhibitors

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