| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
TRC051384 is a novel compound which can potently induce HSPA1A/B (heat shock protein) expression and subsequent Hsp70 production via heat shock factor-1 (HSF1) activation. It has the potential to be developed as a novel pharmacological agent for the treatment of ischemic stroke. RC051384 induces heat shock protein 70 (HSP70) and is a potent anti-inflammatory agent. 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.
| ln Vitro |
TRC051384, in both HeLa and rat primary mixed neurons, dose-dependently increases HSP70B mRNA by several hundred fold. Treatment with TRC051384 causes luciferase activity to recover and HSF1 transcriptional activity to significantly increase in a dose-dependent manner. In differentiated THP-1 cell line, TRC051384 inhibits TNF-α expression induced by LPS by 60% at 6.25 μM and 90% at 12.5 μM[1].
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| ln Vivo |
Even when given eight hours after the onset of ischemia, treatment with TRC051384 significantly reduces stroke associated neuronal injury and disability in a rat model of transient ischemic stroke (87% reduction in area of penumbra recruited to infarct and 25% reduction in brain edema). When TRC051384 medication is started four hours after ischemia onset, there is a significant improvement in survival (50% by day two and 67.3% by day seven). HSF1 activation is required for TRC051384 to induce HSP70, which raises chaperone levels and has anti-inflammatory properties[1].
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| Animal Protocol |
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| References |
| Molecular Formula |
C25H31N5O4
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| Molecular Weight |
465.54
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| Exact Mass |
465.238
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| Elemental Analysis |
C, 64.50; H, 6.71; N, 15.04; O, 13.75
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| CAS # |
867164-40-7
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| Related CAS # |
TRC051384 hydrochloride;1333327-56-2
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| PubChem CID |
11634093
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.734
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
34
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC(NC(NCCN2CCOCC2)=O)=CC=1)C=CC1C=CC=C(N2CCOCC2)N=1
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| InChi Key |
SQTSPANZQDCPLB-CMDGGOBGSA-N
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| InChi Code |
InChI=1S/C25H31N5O4/c31-23(9-8-21-2-1-3-24(27-21)30-14-18-34-19-15-30)20-4-6-22(7-5-20)28-25(32)26-10-11-29-12-16-33-17-13-29/h1-9H,10-19H2,(H2,26,28,32)/b9-8+
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| Chemical Name |
1-(2-morpholin-4-ylethyl)-3-[4-[(E)-3-(6-morpholin-4-ylpyridin-2-yl)prop-2-enoyl]phenyl]urea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1480 mL | 10.7402 mL | 21.4804 mL | |
| 5 mM | 0.4296 mL | 2.1480 mL | 4.2961 mL | |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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