中文名 | USP25 and 28 inhibitor AZ-1 |
英文名 | USP25/28 inhibitor AZ1; AZ1 |
别名 | 化合物AZ1 2-[[[5-溴-2-[[4-氟-3-(三氟甲基)苯基]甲氧基]苯基]甲基]氨基]-乙醇 |
英文别名 | AZ1 AZ-1 AZ 1 USP25 and 28 inhibitor AZ-1 2-((5-bromo-2-((4-fluoro-3-(trifluoromethyl)benzyl)oxy)benzyl)amino)ethanol Ethanol, 2-[[[5-bromo-2-[[4-fluoro-3-(trifluoromethyl)phenyl]methoxy]phenyl]methyl]amino]- |
CAS | 2165322-94-9 |
化学式 | C17H16BrF4NO2 |
分子量 | 422.21 |
密度 | 1.488±0.06 g/cm3(Predicted) |
沸点 | 478.5±40.0 °C(Predicted) |
溶解度 | DMSO : 250 mg/mL (592.12 mM);H2O : < 0.1 mg/mL (不溶) |
酸度系数 | 14.74±0.10(Predicted) |
存储条件 | -20°C |
体内研究 | USP25/28 inhibitor AZ1 (AZ1; 40 mg/kg; gavage; daily; for 7 days) protects from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening. USP25/28 inhibitor AZ1 (20 mg/kg/day; gavage; 6 times a week in the 1, 3, 6 weeks) treatment significantly reduces tumor numbers in colons. Expression of Wnt-related genes and levels of pSTAT3 are decreased and levels of SOCS3 are increased in tumors. AZ1 gavage does not alleviate DSS-induced colitis in Usp25 -/- mice or the spontaneous colitis of Il10 -/- mice. USP25/28 inhibitor AZ1 (20 mg/kg/day; gavage; every 3 days from 13-20 weeks) significantly inhibits tumorigenesis in the colon and prolonged the survival of AOM/Vil-Cre;Trp53 fl/fl (VP) mice. AZ1 treatment has minimal effect on tumorigenesis in the USP25-deficient background. Animal Model: 12-week old male Usp25 +/+ and Usp25 -/- mice Dosage: 40 mg/kg Administration: Gavage; daily; for 7 days Result: Protected from dextran sulfate sodium (DSS)-induced weight loss and diarrhea and impaired colon shortening and potentiated the expression of proinflammatory cytokines and antibacterial peptides in colons of Usp25 -/- mice compared to control counterparts. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.368 ml | 11.842 ml | 23.685 ml |
5 mM | 0.474 ml | 2.368 ml | 4.737 ml |
10 mM | 0.237 ml | 1.184 ml | 2.368 ml |
5 mM | 0.047 ml | 0.237 ml | 0.474 ml |
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