ChemicalBook--->CAS DataBase List--->433249-94-6

433249-94-6

433249-94-6 Structure

433249-94-6 Structure
IdentificationBack Directory
[Name]

6877002
[CAS]

433249-94-6
[Synonyms]

6877002
TRAF-STOP 6877002
CD40-TRAF6 inhibitor
[EINECS(EC#)]

809-295-8
[Molecular Formula]

C17H17NO
[MOL File]

433249-94-6.mol
[Molecular Weight]

251.32
Chemical PropertiesBack Directory
[Boiling point ]

378.6±42.0 °C(Predicted)
[density ]

1.104±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 125 mg/mL (497.37 mM)
[form ]

Solid
[pka]

0.82±0.70(Predicted)
[color ]

Light yellow to yellow
Safety DataBack Directory
[Symbol(GHS) ]


GHS09
[Hazard statements ]

H411
Hazard InformationBack Directory
[Uses]

3-[(2,5-Dimethylphenyl)amino]-1-phenyl-2-propen-1-one functions as CD40-TRAF6 inhibitors. Inhibition of CD40 signalling pathway seems a better way to ameliorate inflammatory diseases, like the inflammation in models of peritonitis and sepsis.
[Biological Activity]

Cell permeable: yes''Primary Target
TRAF6
[in vivo]

TRAF-STOP inhibitor 6877002 (10 μmol/kg; intraperitoneal injection; once a day; 6 weeks) retards the development of early atherosclerosis and reduces atherosclerotic plaque area in apolipoprotein E-deficient (Apoe-/-) mice[1].
TRAF-STOP inhibitor 6877002 (10 μmol/kg; intraperitoneal injection; once a day; 6 weeks) halts the progression of established atherosclerosis, induces a stable plaque phenotype, reduces macrophage number and proliferation, decreases the size of necrotic cores, reduces the number of neutrophils and T cells, and increases collagen and αSMA+ smooth muscle cell content in atherosclerotic plaques in apolipoprotein E-deficient (Apoe-/-) mice[1].
TRAF-STOP inhibitor 6877002 (10 μmol/kg; administered via recombinant high-density lipoprotein nanoparticles; twice a week; 6 weeks) reduces plaque volume in the aortic root and the number of macrophages in plaques in apolipoprotein E-deficient (Apoe-/-) mice[1].

Animal Model:Male apolipoprotein E-deficient (Apoe-/-) mice (22 weeks old), with advanced atherosclerotic lesions already present in the aortic arch to establish an established atherosclerosis model[1].
Dosage:10 μmol/kg (vehicle: PBS, 0.05% Tween 80, 5% dimethylsulfoxide)
Administration:Intraperitoneal injection, once a day, for 6 weeks
Result:Halted the progression of established atherosclerosis, reduced the total atherosclerotic plaque area in the aortic arch and aortic root. The atherosclerotic plaques exhibited a stable phenotype with decreased macrophage number and proliferation, smaller necrotic cores, fewer neutrophils and T cells, and increased collagen and αSMA+ smooth muscle cell content.
Animal Model:Male apolipoprotein E-deficient (Apoe-/-) mice (12 weeks old), fed a normal chow diet to establish an atherosclerosis-prone model[1].
Dosage:10 μmol/kg (vehicle: PBS, 0.05% Tween 80, 5% dimethylsulfoxide)
Administration:Intraperitoneal injection, once a day, for 6 weeks
Result:Retarded the development of early atherosclerosis, reduced atherosclerotic plaque area in the aortic arch, and the plaques contained fewer macrophages, T cells, and neutrophils. There were no changes in the number of proliferating or apoptotic cells, plaque smooth muscle cell or collagen content.
Animal Model:Male apolipoprotein E-deficient (Apoe-/-) mice (12 weeks old) with atherosclerosis model[1].
Dosage:10 μmol/kg (packaged in recombinant high-density lipoprotein nanoparticles)
Administration:Administered via recombinant high-density lipoprotein nanoparticles, twice a week, for 6 weeks
Result:Reduced plaque volume in the aortic root and the number of macrophages in plaques.
[storage]

Store at -20°C
Spectrum DetailBack Directory
[Spectrum Detail]

6877002(433249-94-6)1HNMR
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