Name | Urea, N-[2-(4-morpholinyl)ethyl]-N'-[4-[3-[6-(4-morpholinyl)-2-pyridinyl]-1-oxo-2-propen-1-yl]phenyl] |
---|---|
Synonyms |
1-[2-(Morpholin-4-yl)ethyl]-3-[4-[3-[6-(morpholin-4-yl)pyridin-2-yl]acryloyl]phenyl]urea
TRC 051384 Urea, N-[2-(4-morpholinyl)ethyl]-N'-[4-[3-[6-(4-morpholinyl)-2-pyridinyl]-1-oxo-2-propenyl]phenyl]- TRC051384 |
Description | TRC051384 is a heat shock protein 70 (HSP70) inducer. |
---|---|
Related Catalog | |
Target |
HSP70 |
In Vitro | 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[1]. |
In Vivo | 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[1]. |
Cell Assay | HeLa cell transiently co-transfected with heat shock elements-luciferase reporter and normalization vector, β-galactosidase are treated with vehicle or TRC051384 (12.5 and 25 μM) for 4 hours. Cell lysates are then prepared and analyzed for luciferase and β-galactosidase activity[1]. |
Animal Admin | Rats: Injured hemispheres from vehicle treated animals and TRC051384 treated animals are collected at 10-hour post-initiation of tMCAo. Total RNA from each brain sample is extracted followed by cDNA preparation. Each sample of cDNA is analyzed[1]. |
References |
Molecular Formula | C25H31N5O4 |
---|---|
Molecular Weight | 465.54500 |
Exact Mass | 465.23800 |
PSA | 96.03000 |
LogP | 2.73480 |
Storage condition | -20℃ |