| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Tau aggregation[1]
Tau protein. BSc3094 interacts closely with the tau protein at the edge involving protons I-IV, while a second attachment site seems to be at the nitro group. It binds to tau and stabilizes its native conformation, preventing beta-sheet formation and aggregation. |
|---|---|
| ln Vitro |
BSc3094 inhibits tau aggregation and dissolves preformed tau paired helical filaments (PHFs) in cell-free assays. It has been shown to reduce sarkosyl-insoluble tau levels and exhibit low cytotoxicity while enhancing cell viability in tauopathy cell models.
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| ln Vivo |
Sarkosyl-insoluble Tau is decreased by direct intraventricular injection of BSc3094 (3 mg/kg)[1]. By restoring the paired-pulse depression seen in pro-aggregant Tau slices that were not treated following the application of a paired-pulse stimulus of the Schaffer collaterals, BSc3094 rescues the pre-synaptic deficit in organotypic hippocampus slices from pro-aggregant animals. In rTg4510 mice, BSc3094 restores the increase in Tau phosphorylation levels to the baseline level. In rTg4510 mice, BSc3094 partially improved memory deficits[1].
BSc3094 administered by direct intraventricular injection (3 mg/kg; i.v.) reduces sarkosyl-insoluble tau levels in vivo, demonstrating that it can effectively target and clear pathological tau aggregates in the brain. This supports its potential as a therapeutic agent to reverse tau pathology. |
| Enzyme Assay |
Recombinant tau protein is incubated with heparin (10 uM) in aggregation buffer (50 mM Tris-HCl, pH 7.4) in the presence or absence of BSc3094. For PHF dissolution assays, pre-formed tau PHFs are generated by prolonged agitation of tau protein (4 days at 37degC), then incubated with BSc3094. Aggregation is monitored by ThT fluorescence (excitation 440 nm, emission 480 nm). IC50 values are determined by curve fitting.
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| Cell Assay |
Human neuroblastoma cell lines (e.g., SH-SY5Y or BE(2)-M17) expressing tau protein are treated with BSc3094 at various concentrations (0.075 to 10 uM) for 24-48 hours. Cell viability is assessed by MTT assay. Levels of sarkosyl-insoluble tau and total tau are quantified by Western blot. Aggregated tau is visualized by immunocytochemistry with anti-tau antibodies to assess reduction of tau pathology.
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| Animal Protocol |
Animal/Disease Models: Mice[1]
Doses: 3 mg/kg Route of Administration: Iv Experimental Results: Direct intraventricular administration decreased sarkosyl-insoluble Tau. Animal/Disease Models: rTg4510 mice[1] Doses: 0.075~1.5 mM Route of Administration: Intraventricular administration Experimental Results: decreased the levels of sarkosyl-insoluble Tau in cortical extracts by ≈70%. For efficacy studies, mice are administered BSc3094 via intraventricular injection at 3 mg/kg. For pharmacokinetics, intravenous administration (3 mg/kg) via tail vein is performed. Brain and plasma samples are collected at various time points post-injection (0.5, 1, 2, 4, 8, 24 hours). Brain homogenates are prepared and sarkosyl-insoluble tau levels are quantified by ELISA or Western blot. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for BSc3094 are limited. The compound is typically administered intravenously or intraventricularly due to expected poor blood-brain barrier penetration. Its molecular weight (380.38) is moderate, and in vitro stability assays suggest it can reach brain tissue following direct CNS administration as demonstrated in rodent models.
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| Toxicity/Toxicokinetics |
BSc3094 displays low cytotoxicity in cell models at concentrations up to 10 uM. At 1 and 4 hours of treatment, it shows minimal toxic effects on cell viability while significantly reducing tau aggregation. No acute toxicity or adverse events have been reported in animal studies at the tested dose (3 mg/kg, i.v., intraventricular).
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| References | |
| Additional Infomation |
Other information: BSc3094 belongs to the N-phenylamine derivative class. Its unique ability to dissolve pre-formed tau PHFs distinguishes it from inhibitors that only prevent new aggregate formation, offering potential for clearance of existing pathology. It is a research chemical not approved for clinical use.
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| Molecular Formula |
C17H12N6O3S
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|---|---|
| Molecular Weight |
380.38
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| Exact Mass |
380.069
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| CAS # |
946857-84-7
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| PubChem CID |
25096749
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| Appearance |
Yellow to orange solid powder
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| LogP |
4.338
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
553
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C2=CSC(=N2)NNC(=O)C3=CC4=C(C=C3)N=CN4)[N+](=O)[O-]
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 33.33 mg/mL (87.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 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 | 2.6289 mL | 13.1447 mL | 26.2895 mL | |
| 5 mM | 0.5258 mL | 2.6289 mL | 5.2579 mL | |
| 10 mM | 0.2629 mL | 1.3145 mL | 2.6289 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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