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Telotristat etiprate

Time:2016-11-01

Telotristat_Etiprate_structure

CAS#: 1137608-69-5 (etiprate)

Description: Telotristat etiprate, its free base also known as LX1606 or LX1032, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor . Telotristat etiprate has activity in controlling diarrhea associated with carcinoid syndrome. LX1606 acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. TPH is the rate-limiting enzyme involved in serotonin biosynthesis and is present in metastatic carcinoid tumor cells.

Synonym: LX1032 etiprate; LX1032 etiprate; LX 1032 etiprate; LX1606; LX1606 etiprate; LX 1606; LX 1606 Hippurate; Telotristat etiprate;

IUPAC/Chemical Name: (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate 2-benzamidoacetate .

THEORETICAL ANALYSIS

Name: Telotristat etiprate
CAS#: 1137608-69-5 (etiprate)
Chemical Formula: C36H35ClF3N7O6
Exact Mass:
Molecular Weight: 754.16
Elemental Analysis: C, 57.33; H, 4.68; Cl, 4.70; F, 7.56; N, 13.00; O, 12.73

TECHNICAL DATA

Appearance:
white solid powder
Purity:
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility:
Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 – 4 C for short term (days to weeks), or -20 C for long term (months).

 

ADDITIONAL INFORMATION

Related CAS#
CAS#1033805-22-9 (Telotristat ethyl)
CAS#1033805-28-5 (Telotristat)
CAS#1137608-69-5 (Telotristat etiprate)

REFERENCES

1: Kulke MH, O’Dorisio T, Phan A, Bergsland EK, Law L, Banks P, Freiman J, Frazier K, Jackson J, Yao JC, Kvols L, Lapuerta P, Zambrowicz B, Fleming D, Sands A. Telotristat etiprate in carcinoid syndrome not adequately controlled by octreotide. Endocr Relat Cancer. 2014 Jul 10. pii: ERC-14-0173. [Epub ahead of print] PubMed PMID: 25012985.

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