| Identification | Back Directory | [Name]
TRC051384 | [CAS]
867164-40-7 | [Synonyms]
TRC051384
TRC 051384; TRC-051384
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]- | [Molecular Formula]
C25H31N5O4 | [MDL Number]
MFCD28133369 | [MOL File]
867164-40-7.mol | [Molecular Weight]
465.54 |
| Chemical Properties | Back Directory | [Boiling point ]
685.7±55.0 °C(Predicted) | [density ]
1.260±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥109 mg/mL in DMSO | [form ]
solid | [pka]
13.47±0.46(Predicted) | [color ]
Yellow |
| Hazard Information | Back Directory | [Uses]
N-[2-(4-Morpholinyl)ethyl]-N''-[4-[3-[6-(4-morpholinyl)-2-pyridinyl]-1-oxo-2-propen-1-yl]phenyl]urea is a key reactant in the synthesis of TRC051384, which is a small molecule HSP70 inducer. | [Biological Activity]
trc 051384, belonging to substituted 2-propen-1-one class, is a potent inducer of heat shock protein 70 (hsp70) [1]. induction of hsp70 is a natural response of stressed cells that protects neuronal cells from a variety of insults including acute ischemia. therefore, induction of hsp70 provides a potential target for the treatment of stroke [1]. | [in vitro]
induction of hsp70 by trc 051384 (6.25, and 12.5 μm) involved heat shock factor-1 (hsf1) activation in hela cells and led to increasing chaperone and anti-inflammatory activity [1]. moreover, trc 051384 (10-50 μm) dose-dependently induced hspa1b overexpression in endothelial cells as well as leucocyte origin [2]. | [in vivo]
trc 051384 (9 mg/kg, intra-peritoneal administration) treatment significantly decreased stroke-associated neuronal injury, disability, and increased survival in a rat model of transient ischemic stroke [1]. in addition, trc 051384 (9 mg/kg, intra-peritoneal administration) delayed thrombus formation without increasing bleeding risk in wt mice [2]. | [target]
hsp70 | [IC 50]
HSP70 | [References]
1. mohanan a, deshpande s, jamadarkhana pg, kumar p, gupta rc, chauthaiwale v, et al. delayed intervention in experimental stroke with trc 051384--a small molecule hsp70 inducer. neuropharmacology. 2011;60(6):991-9. 2. allende m, molina e, guruceaga e, tamayo i, gonzalez-porras jr, gonzalez-lopez tj, et al. hsp70 protects from stroke in atrial fibrillation patients by preventing thrombosis without increased bleeding risk. cardiovasc res. 2016;110(3):309-18. |
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BOC Sciences
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