ChemicalBook CAS DataBase List 433249-94-6

433249-94-6

Name	6877002
CAS	433249-94-6
EINECS(EC#)	809-295-8
Molecular Formula	C17H17NO
Molecular Weight	251.32
MOL File	433249-94-6.mol

Chemical Properties

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 Data

Symbol(GHS)	GHS09
Hazard statements	H411

Hazard Information

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 Detail

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