中文名 | TRC051384 |
英文名 | TRC051384 |
别名 | TRC051384游离态 化合物TRC 051384 1-(2-吗啉乙基)-3-(4-(3-(6-吗啉吡啶-2-基)丙烯酰基)苯基)脲 |
英文别名 | TRC051384 TRC 051384 TRC-051384 1-(2-Morpholinoethyl)-3-(4-(3-(6-morpholinopyridin-2-yl)acryloyl)phenyl)urea N-[2-(4-Morpholinyl)ethyl]-N'-[4-[3-[6-(4-morpholinyl)-2-pyridinyl]-1-oxo-2-propen-1-yl]phenyl]urea Urea, N-[2-(4-morpholinyl)ethyl]-N'-[4-[3-[6-(4-morpholinyl)-2-pyridinyl]-1-oxo-2-propen-1-yl]phenyl]- |
CAS | 867164-40-7 |
化学式 | C25H31N5O4 |
分子量 | 465.54 |
密度 | 1.260±0.06 g/cm3(Predicted) |
沸点 | 685.7±55.0 °C(Predicted) |
溶解度 | 溶于DMSO |
酸度系数 | 13.47±0.46(Predicted) |
存储条件 | -20℃ |
体外研究 | TRC051384, dose dependently induces HSP70B mRNA by several hundred folds in both HeLa and rat primary mixed neurons. Treatment with TRC051384 results in significant dose-dependent increase in HSF1 transcriptional activity and recovery of luciferase activity. TRC051384 results in 60% inhibition at 6.25 μM and 90% inhibition at 12.5 μM of LPS-induced TNF-α expression in differentiated THP-1 cell line. |
体内研究 | Treatment with TRC051384 significantly reduces stroke associated neuronal injury (87% reduction in area of penumbra recruited to infarct, and 25% reduction in brain edema) and disability in a rat model of transient ischemic stroke even when administered 8 hours post onset of ischemia. Significant improvement in survival (50% by day2 and 67.3% by day 7) is observed with TRC051384 treatment initiated at 4 hours after ischemia onset. Induction of HSP70 by TRC051384 involves HSF1 activation and results in elevated chaperone and anti-inflammatory activity. |
参考资料 展开查看 | 1. Mohanan et al (2011) Delayed intervention in experimental stroke with TRC051384--a small molecule HSP70 inducer. Neuropharmacology. 60 991. PMID: 21167846. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.148 ml | 10.74 ml | 21.48 ml |
5 mM | 0.43 ml | 2.148 ml | 4.296 ml |
10 mM | 0.215 ml | 1.074 ml | 2.148 ml |
5 mM | 0.043 ml | 0.215 ml | 0.43 ml |
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