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SEN-177

Names

[ CAS No. ]:
2117405-13-5

[ Name ]:
SEN-177

[Synonym ]:
3',3'']terpyridine
SEN177
MFCD30343871
Piperidine, 1-(6'-fluoro[3,3'-bipyridin]-2-yl)-4-(4-methyl-4H-1,2,4-triazol-3-yl)-
6'-Fluoro-2-[4-(4-methyl-4H-1,2,4-triazol-3-yl)-1-piperidinyl]-3,3'-bipyridine
6''-Fluoro-4-(4-methyl-4H-[1,2,4]triazol-3-yl)-3,4,5,6-tetrahydro-2H-[1,2'
6''-fluoro-4-(4-methyl-4H-[1,2,4]triazol-3-yl)-3,4,5,6-tetrahydro-2H-[1,2';3',3'']terpyridine

Biological Activity

[Description]:

SEN177 is an inhibitor of glutaminyl cyclase (QPCT), thereby rescuing the Huntington's disease (HD)-related phenotypes in cell.

[In Vitro]

SEN177 is a Glutaminyl cyclase (QPCT) inhibitor. Glutaminyl cyclase modifies N-terminal glutamine or glutamate residues to N-terminal 5-oxoproline or pyroglutamate (named QPCT). QPCT inhibits mutant huntingtin from forming aggregates, but also reduces aggregation of other aggregate-prone proteins containing polyQ or polyA repeats. SEN177 caused dose-dependent decreases in HTT aggregation by a mechanism that requires QPCT inhibition. SEN177 had in vitro activity against polyglutamine toxicity and was able to reduce aggregates in mammalian cells, primary neurons and in a Drosophila model.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
581.3±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C18H19FN6

[ Molecular Weight ]:
338.382

[ Flash Point ]:
305.3±32.9 °C

[ Exact Mass ]:
338.165527

[ LogP ]:
1.12

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.683

Related Compounds