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BOC Sciences |
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| | 6877002 Basic information |
| Product Name: | 6877002 | | Synonyms: | 6877002;TRAF-STOP 6877002;2-Propen-1-one, 3-[(2,5-dimethylphenyl)amino]-1-phenyl-;Compound 6877002;Compound 6877002, CD40-TRAF6 interaction inhibitor;TRAF-STOP inhibitor 6877002, 10 mM in DMSO;CD40-TRAF6 inhibitor;CD40-TRAF6 signaling inhibitor | | CAS: | 433249-94-6 | | MF: | C17H17NO | | MW: | 251.32 | | EINECS: | 809-295-8 | | Product Categories: | | | Mol File: | 433249-94-6.mol |  |
| | 6877002 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) | | pka | 0.82±0.70(Predicted) | | form | Solid | | color | Light yellow to yellow | | InChI | 1S/C16H15NO/c1-12-8-9-13(2)15(10-12)17-11-16(18)14-6-4-3-5-7-14/h3-11H,1-2H3/b17-11+ | | InChIKey | WIFPLULEUNBSTE-GZTJUZNOSA-N | | SMILES | O=C(C1=CC=CC=C1)/C=N/C2=CC(C)=CC=C2C |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | 6877002 Usage And Synthesis |
| 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 +4°C |
| | 6877002 Preparation Products And Raw materials |
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