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ACT-678689

Names

[ CAS No. ]:
1783256-96-1

[ Name ]:
ACT-678689

[Synonym ]:
N-(6-Chloro-5-{2-[(5S)-5-(2-fluoro-4-methylphenyl)-2-methyl-7,8-dihydro[1,3,4]thiadiazolo[2',3':2,3]imidazo[4,5-c]pyridin-6(5H)-yl]-2-oxoethoxy}-2-pyridinyl)methanesulfonamide
Methanesulfonamide, N-[6-chloro-5-[2-[(5S)-5-(2-fluoro-4-methylphenyl)-7,8-dihydro-2-methyl-1,3,4-thiadiazolo[2',3':2,3]imidazo[4,5-c]pyridin-6(5H)-yl]-2-oxoethoxy]-2-pyridinyl]-

Biological Activity

[Description]:

ACT-678689 (Compound Example 1.53.4) is a tryptophan hydroxylase (TPH) inhibitor with an IC50 of 8 nM[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Tryptophan Hydroxylase
Research Areas >> Inflammation/Immunology

[Target]

IC50: 8 nM (TPH)[1]


[In Vitro]

TPH comprises two isoforms: TPH2 is mainly expressed in neuronal cell types in the central nervous system (CNS), while TPH1 is mainly expressed in peripheral tissues, including the entrochromaffin cells (EC) in the gut, where it is responsible for synthesizing 5HT that is stored in circulating blood platelets[1].

[References]

[1]. Daniel Bur, et al. Tricyclic piperidine compounds. WO2015075023A1.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C23H22ClFN6O4S2

[ Molecular Weight ]:
565.040

[ Exact Mass ]:
564.081665

[ LogP ]:
2.15

[ Index of Refraction ]:
1.734

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xn


Related Compounds