| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
tau and α-syn[1]
Monomeric tau and alpha-synuclein (alpha-syn). MG-2119 binds to these monomeric proteins, preventing their conformational change and subsequent aggregation into toxic oligomers and fibrils. |
|---|---|
| ln Vitro |
MG-2119 inhibits tau and alpha-syn aggregation in thioflavin T (ThT) fluorescence assays. It also rescues combined tau and alpha-syn-induced cytotoxicity in SH-SY5Y neuroblastoma cells in a dose-dependent manner, demonstrating neuroprotective effects.
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| ln Vivo |
In vivo activity data for MG-2119 are limited. Given its potent in vitro activity and rescue of cellular cytotoxicity, it is hypothesized to reduce protein aggregation and associated neurotoxicity in animal models of neurodegeneration, though this has not been fully characterized in published literature to date.
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| Enzyme Assay |
Recombinant tau protein (2 uM) or alpha-synuclein is incubated with heparin (10 uM) in aggregation buffer (50 mM Tris-HCl, 100 mM NaCl, pH 7.4) in the presence or absence of MG-2119 (0.1-100 uM). Thioflavin T (ThT, 20 uM) is added to monitor fibril formation. Fluorescence (excitation 440 nm, emission 480 nm) is measured kinetically at 37degC to assess lag time and elongation rate.
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| Cell Assay |
Human SH-SY5Y neuroblastoma cells are co-transfected with tau and alpha-synuclein expression plasmids to model dual protein aggregation. After 24 hours, cells are treated with increasing concentrations of MG-2119 (0.1-50 uM) for another 24-48 hours. Cell viability is assessed by MTT or CCK-8 assay. Aggregates are visualized by immunocytochemistry using anti-tau and anti-alpha-syn antibodies.
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| Animal Protocol |
No specific in vivo animal experimental protocols are widely published for MG-2119. Studies would likely use transgenic mouse models of tauopathy (e.g., Tau-P301S) or synucleinopathy (e.g., alpha-syn A53T). Compound would be administered intraperitoneally (10-30 mg/kg) daily for 4-8 weeks, followed by histopathological analysis for protein aggregates in brain sections and behavioral assessments.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties have not been fully characterized for MG-2119. Based on its molecular weight of 487.55 and chemical structure, it may have moderate oral bioavailability. DMSO (100 mg/mL) solubility is reported, with aqueous solubility likely low, requiring formulation with co-solvents for in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicology data for MG-2119 are not available in the literature. As an investigational compound, it would require standard safety pharmacology studies (hERG, Ames, etc.) before progression. In cellular assays, it rescues cytotoxicity rather than inducing it, suggesting a favorable safety profile at active concentrations.
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| References | |
| Additional Infomation |
Other information: MG-2119 is unique as a dual inhibitor of both tau and alpha-synuclein aggregation, making it a promising tool for studying overlapping proteinopathies in neurodegenerative diseases. It is not yet FDA-approved and is strictly a research-grade chemical.
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| Molecular Formula |
C27H29N5O4
|
|---|---|
| Molecular Weight |
487.55
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| Exact Mass |
487.221
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| CAS # |
1065500-40-4
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| PubChem CID |
45183711
|
| Appearance |
White to light yellow solid powder
|
| LogP |
2.7
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
36
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| Complexity |
704
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(=CC(C(NCC(C)OC2C=CC=NC=2)=O)=C2C(=C1)N=CN2CCC1=CC=CC=C1)NC(COC)=O
|
| InChi Key |
BQOOSSSSVKDEIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H29N5O4/c1-19(36-22-9-6-11-28-16-22)15-29-27(34)23-13-21(31-25(33)17-35-2)14-24-26(23)32(18-30-24)12-10-20-7-4-3-5-8-20/h3-9,11,13-14,16,18-19H,10,12,15,17H2,1-2H3,(H,29,34)(H,31,33)
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| Chemical Name |
6-[(2-methoxyacetyl)amino]-3-(2-phenylethyl)-N-(2-pyridin-3-yloxypropyl)benzimidazole-4-carboxamide
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 100 mg/mL (205.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.13 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 (5.13 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0511 mL | 10.2554 mL | 20.5107 mL | |
| 5 mM | 0.4102 mL | 2.0511 mL | 4.1021 mL | |
| 10 mM | 0.2051 mL | 1.0255 mL | 2.0511 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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