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6,6-DIMETHYL-3-(5-METHYL-3-OXO-2-(4-(TRIFLUOROMETHOXY)PHENYL)-2,3-DIHYDRO-1H-PYRAZOL-4-YL)-1-PHENYL-3-(TRIFLUOROMETHYL)-6,7-DIHYDRO-1H-INDOLE-2,4(3H,5H)-DIONE

Names

[ CAS No. ]:
1067647-43-1

[ Name ]:
6,6-DIMETHYL-3-(5-METHYL-3-OXO-2-(4-(TRIFLUOROMETHOXY)PHENYL)-2,3-DIHYDRO-1H-PYRAZOL-4-YL)-1-PHENYL-3-(TRIFLUOROMETHYL)-6,7-DIHYDRO-1H-INDOLE-2,4(3H,5H)-DIONE

Biological Activity

[Description]:

ELOVL6-IN-2 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-2 inhibits mouse ELOVL6 activities, with an IC50 value of 34 nM[1].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[Target]

IC50: 34 nM (ELOVL6)[1]


[In Vivo]

ELOVL6-IN-2 (0.1~1mg/kg; p.o.; 2 hours) potently and dose-proportionally suppresses the elongation index in the liver[1]. ELOVL6-IN-2 (10mg/kg; p.o.; 2 hours) demonstrates highly liver penetrable[1]. ELOVL6-IN-2 (1mg/kg; p.o.; 2~24 hours) exhibits sustained plasma exposure[1]. Animal Model: Male C57BL/6J mice Dosage: 0.1~1mg/kg Administration: P.o Result: Potently and dose-proportionally suppressed the elongation index in the liver. Animal Model: Male C57BL/6J mice Dosage: 10 mg/kg Administration: P.o Result: Demonstrated highly liver penetrable. Animal Model: Male C57BL/6J mice Dosage: 1 mg/kg Administration: P.o Result: Exhibited sustained plasma exposure.

[References]

[1]. akahashi T, et al. Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors. J Med Chem. 2009;52(10):3142-3145.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H23F6N3O4

[ Molecular Weight ]:
579.49000

[ Exact Mass ]:
579.15900

[ PSA ]:
84.40000

[ LogP ]:
5.92770

[ Storage condition ]:
-20°C