| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| ln Vitro |
PBA-1105 TFA induced autophagic degradation of stably expressed mutant tau protein at a median lethal concentration (DC50) of 0.71 nM and a maximum lethal concentration (Dmax, 24 hr) of 100 nM, with a hook effect at higher concentrations [1]. PBA-1105 (0.1–10 μM; 24 h) TFA induced autophagic degradation of misfolded proteins and aggregates at nanomolar concentrations. PBA-1105 TFA significantly degraded mutant tau protein and misfolded protein [1].
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| ln Vivo |
PBA-1105 (20-50 mg/kg; intraperitoneal injection; three times a week; for 4 weeks) TFA successfully reduced tau aggregates and oligomer types in a transgenic mouse tau disease model [1].
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| Cell Assay |
Western Blot analysis [1]
Cell Types: HEK293T cells Tested Concentrations: 1 μM Incubation Duration: 24 hours Experimental Results: Activated p62 oligomerization and increased autophagy flux of ubiquitinated aggregates. Western Blot Analysis [1] Cell Types: SH-SY5Y-tauP301L cells Tested Concentrations: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 2.5 μM, 5 μM, 10 μM Incubation Duration: 24 hours Experimental Results: Selectively degraded the mutant tauP301L, with a DC50 of 0.71 nM, and continuously cleared insoluble tau aggregates. |
| Animal Protocol |
Animal/Disease Models:hTauP301L-BiFC transgenic mice [1]
Doses: 20 mg/kg or 50 mg/kg (PBS containing 30% polyethylene glycol (PEG)) Route of Administration: Intraperitoneal injection; three times a week for 4 weeks Experimental Results: Effectively cleared tau protein aggregates in a dose-dependent manner, significantly reduced insoluble tau protein in the brain, but had no effect on soluble tau protein. Increased levels of autophagy markers such as LC3, confirming the activation of the autophagy degradation pathway. Immunohistochemical analysis showed that tau oligomers and phosphorylated tau protein were significantly reduced in the cortex and hippocampus. |
| References |
| Molecular Formula |
C41H49F3N2O8
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|---|---|
| Molecular Weight |
754.83
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| Appearance |
Colorless to light yellow oil
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| SMILES |
O=C(O)C(F)(F)F.O=C(CCCC1=CC=CC=C1)NCCOCCOCCOCCNCC2=CC(OCC3=CC=CC=C3)=C(OCC4=CC=CC=C4)C=C2
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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: 请将本产品存放在密封保护的环境中，避免受潮。 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3248 mL | 6.6240 mL | 13.2480 mL | |
| 5 mM | 0.2650 mL | 1.3248 mL | 2.6496 mL | |
| 10 mM | 0.1325 mL | 0.6624 mL | 1.3248 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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