TRC051384 是热休克蛋白 HSP70 的诱导剂，可激活热休克因子-1 并增强神经元和神经胶质细胞中 HSP72 的表达。

TRC051384 is an inducer of heat shock protein Hsp70, activating heat shock factor-1 and enhancing Hsp72 expression in neurons and glial cells.

TRC051384, a novel compound belonging to substituted 2-propen-1-one class is a potent inducer of heat shock protein 70 (HSP70).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 day 2 and 67.3% by day 7) was 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.?These results show that TRC051384 has the potential to be developed as a novel pharmacological agent for the treatment of ischemic stroke.

Focal cerebral ischemia was produced in rats by occluding the MCA using the intra luminal suture technique.?Rats subjected to 2 hours focal cerebral ischemia were administered by intra-peritoneal route, TRC051384 or vehicle every 2 hours for 48 hours, from 4th hour or 8th hour after onset of ischemia.?Progression of infarct and edema was assessed up to 48 hours post ischemic insult using magnetic resonance imaging and the neurological disability and survival studied till 7 days.

1333327-56-2

C25H32ClN5O4

502

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years