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| ln Vitro |
Synucleozid (0.25-1 μM; 24 hours) eliminates the cytotoxicity caused by produced fibrils of α-synuclein, which function as seeds and attract endogenous α-synuclein to aggregate[1]. Synucleozid (0-1 μM; 24 hours) inhibits the expression of α-synuclein protein in SH-SY5Y neuroblastoma cells and binds to the A bulge near the base of the IRE hairpin. It also reduces α-synuclein levels in a dose-dependent manner with an IC50 of 500 nM[1]. Similar affinities are seen in the binding of synucleozid (100 nM–100 μM; 24 hours) to both natural and 2-AP-labeled IRE RNA. It reduces 2-AP emission with an EC50 value of 2.7 ± 0.4 μM. Recovery of 2-AP emissions is shown in relation to the concentration of unlabeled SNCA IRE RNA (RNA-0), providing a competitive Kd of 1.5 ± 0.3 μM[1]. In a dose-dependent manner, synucleozid (0.25-1 μM; 24 hours) reduces α-synuclein and other proteins with IREs in their mRNA's UTR, such as APP, PrP, Ferritin, and TfR. Except for the PrP protein, which is evaluated in Neuro-2A cells, all panels are finished in SH-SY5Y cells[1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: SH-SY5Y neuroblastoma cells Tested Concentrations: 0.25 μM, 0.5 μM, 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished LDH release as a dose-dependent manner. Western Blot Analysis[1] Cell Types: SH-SY5Y neuroblastoma cells Tested Concentrations: 0.25 μM, 0.5 μM, 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished α-synuclein expression as a concentration-dependent manner. |
| References |
[1]. Zhang P, et al. Translation of the intrinsically disordered protein α-synuclein is inhibited by a small molecule targeting its structured mRNA.Proc Natl Acad Sci U S A. 2020 Jan 21;117(3):1457-1467.
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| Molecular Formula |
C22H21CLN6
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| Molecular Weight |
404.90
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| Exact Mass |
404.15
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| CAS # |
2741856-68-6
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| Related CAS # |
Synucleozid;502139-01-7
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| Appearance |
Powder
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| SMILES |
C1=CC(=CC=C1C2=CC3=C(N2)C=C(C=C3)C(=N)N)NC4=CC=C(C=C4)C(=N)N.Cl
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| InChi Key |
GKVDOKIPCRSEMM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20N6.ClH/c23-21(24)14-5-9-18(10-6-14)27-17-7-3-13(4-8-17)19-11-15-1-2-16(22(25)26)12-20(15)28-19;/h1-12,27-28H,(H3,23,24)(H3,25,26);1H
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| Chemical Name |
2-[4-(4-carbamimidoylanilino)phenyl]-1H-indole-6-carboximidamide;hydrochloride
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| Synonyms |
NSC 377363 hydrochloride; Synucleozid hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~125 mg/mL (~308.7 mM)
H2O : ~2 mg/mL (~5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.14 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 20.8 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: ≥ 2.08 mg/mL (5.14 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 20.8 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 | 2.4697 mL | 12.3487 mL | 24.6975 mL | |
| 5 mM | 0.4939 mL | 2.4697 mL | 4.9395 mL | |
| 10 mM | 0.2470 mL | 1.2349 mL | 2.4697 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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