Telotristat

Modify Date: 2024-01-02 19:15:59

Telotristat Structure
Telotristat structure
Common Name Telotristat
CAS Number 1033805-28-5 Molecular Weight 546.92900
Density 1.50±0.1 g/cm3 (20 ºC 760 Torr), 计算值 Boiling Point N/A
Molecular Formula C25H22ClF3N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Telotristat


Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.

 Names

Name Telotristat
Synonym More Synonyms

 Telotristat Biological Activity

Description Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
Related Catalog
Target

IC50: 0.028 μM (tryptophan hydroxylase)[1]

In Vitro Telotristat is the active moiety of telotristat etiprate. Telotristat etiprate is an ethyl ester prodrug which is hydrolyzed to telotristat. Telotristat etiprate is orally available serotonin synthesis inhibitor for the treatment of carcinoid syndrome[1].
In Vivo Telotristat etiprate is present in very low levels after oral administration. These low levels are due to rapid hydrolysis into the active moiety telotristat. The half-life ranges from approximately 4-12 h. There is no accumulation of telotristat with multiple dose administration over 2 weeks. Exposure to telotristat is approximately dose proportional[1].
Cell Assay BON CBA cells are grown in equal volume of DMEM and F12K with 5% bovine serum for 3-4 hours (20 K cell/well) and telotristat is added at a concentration range of 0.07 to 50 μM. The cells are incubated at 37°C overnight. 50 μM of the culture supernatant is then taken for 5HTP measurement. The supernatant is mixed with equal volume of 1M TCA, then filtered through glass fiber. The filtrate is loaded on reverse phase HPLC for 5HTP concentration measurement. The cell viability is measured by treating the remaining cells with Celltiter-Glo Luminescent Cell Viability Assay[2].
Animal Admin Rats: 14-week-old male C57 albino mice are dosed once daily by oral gavage at 5-10 mL/kg for four consecutive days. Five hours after the last dose, the animals are quickly sacrificed. 5-HT is extracted from the blood or tissues and measured by HPLC. Blood samples are taken for exposure analysis[2].
References

[1]. Lapuerta P, et al. Telotristat etiprate, a novel inhibitor of serotonin synthesis for the treatment of carcinoid syndrome. Clin. Invest. (Lond.) (2015) 5(5), 447–456

[2]. US20080153852

 Chemical & Physical Properties

Density 1.50±0.1 g/cm3 (20 ºC 760 Torr), 计算值
Molecular Formula C25H22ClF3N6O3
Molecular Weight 546.92900
Exact Mass 546.13900
PSA 142.17000
LogP 5.79160
Storage condition 2-8℃

 Precursor & DownStream

Precursor  0

DownStream  1

 Synonyms

LP778902
(S)-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)propanoic acid
(S)-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)propanoic acid
(S)-2-amino-3-[4-(2-amino-6-{(R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy}pyrimidine-4-yl)phenyl]propionic acid
(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]propanoic acid
Top Suppliers:I want be here



Get all suppliers and price by the below link:

Telotristat suppliers


Price: $303/10mM*1mLinDMSO

Reference only. check more Telotristat price