Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
ln Vitro |
A dose-dependent reduction in the REST isoform in protein level is induced by X5050 (100 µM, 1 day)[1].
|
---|---|
ln Vivo |
In the pathogenic context of HD, X5050 (2 x 2µl of 20 mM) exhibits activity[1].
|
Cell Assay |
Western Blot Analysis[1]
Cell Types: NSCs. Tested Concentrations: 100 µM. Incubation Duration:One day. Experimental Results: Induced a dosedependent decrease in the 122 kDa longer REST isoform. |
Animal Protocol |
Animal/Disease Models: 12weeks old male C57Bl6 mice[1].2
Doses: 2 x 2µl of 20 mM in 10% DMSO in water. Route of Administration: Intraventricular injection. Experimental Results: Increased BDNF expression. A decrease in Darpp32 and Snap25 expression was found by QRT-PCR in the lesioned striatum as compared with the contralateral striatum. Dramatically increased the levels of Bdnf II splice variant (exon II containing variant) while Bdnf IV levels were not Dramatically changed. |
References |
[1]. Jérémie Charbord, et al. High throughput screening for inhibitors of REST in neural derivatives of human embryonic stem cells reveals a chemical compound that promotes expression of neuronal genes. Stem Cells. 2013 Sep;31(9):1816-28.
|
Molecular Formula |
C17H15N3O3
|
---|---|
Molecular Weight |
309.32
|
CAS # |
2404756-81-4
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O([H])C1=C([H])C([H])=C([H])C([H])=C1C1=NC2C([H])=C([H])C(C(N([H])OC([H])([H])C([H])=C([H])[H])=O)=C([H])C=2N1[H]
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 100 mg/mL (323.29 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2329 mL | 16.1645 mL | 32.3290 mL | |
5 mM | 0.6466 mL | 3.2329 mL | 6.4658 mL | |
10 mM | 0.3233 mL | 1.6164 mL | 3.2329 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.