| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Aberrant tau ligand 1 targets tau proteins that have acquired abnormal (misfolded) conformations. It selectively binds to pathogenic tau species and serves as a warhead to direct PROTAC molecules to aberrant tau for ubiquitination and proteasomal degradation. It does not target normal tau in published reports.
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|---|---|
| ln Vitro |
Aberrant tau ligand 1 alone has no direct degradation activity. When conjugated into a PROTAC such as QC‑01‑175, it enables selective degradation of aberrant tau in patient‑derived neuronal cell models. The ligand contributes to the formation of a ternary complex with tau and an E3 ligase, facilitating ubiquitination of tau.
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| ln Vivo |
Aberrant tau ligand 1 itself has no in vivo degradation activity. PROTACs containing aberrant tau ligand 1 (e.g., QC‑01‑175) have been evaluated in frontotemporal dementia patient‑derived neuronal cell models, but specific animal model data for the ligand alone are not reported. The PROTAC degrader is designed for in vivo tau reduction studies.
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| Enzyme Assay |
Binding of aberrant tau ligand 1 to misfolded tau is typically confirmed by surface plasmon resonance (SPR) or fluorescence polarization (FP) assays using purified recombinant tau aggregates. The ligand is incubated with immobilized tau species, and KD is calculated from saturation binding curves. No specific KD value is reported.
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| Cell Assay |
Patient‑derived frontotemporal dementia (FTD) neurons carrying tau mutations are cultured in 96‑well plates. Cells are treated with a PROTAC containing aberrant tau ligand 1 at graded concentrations for 24‑72 h, then lysed. Tau protein levels are quantified by Western blot or ELISA using antibodies specific to total tau or phosphorylated tau isoforms.
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| Animal Protocol |
For in vivo evaluation of a PROTAC degrader containing aberrant tau ligand 1, tauopathy model mice (e.g., PS19 or rTg4510) are treated intraperitoneally or orally with the PROTAC compound for several weeks. Brain tissues are collected post‑treatment, and tau pathology is assessed by immunohistochemistry and biochemical fractionation to measure soluble and insoluble tau species.
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| ADME/Pharmacokinetics |
Aberrant tau ligand 1 is soluble in DMSO at 12.5 mg/mL (52.03 mM). The ligand can be stored as a powder at 4degC protected from light. For in vitro use, stock solutions in DMSO are stored at ‑80degC for up to 6 months or at ‑20degC for 1 month. No specific PK data are available.
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| Toxicity/Toxicokinetics |
No direct toxicity data are reported for aberrant tau ligand 1. As a research tool for PROTAC development, it is not intended for human use. Standard safety precautions for chemical handling should be observed. The compound has not undergone formal toxicological testing for therapeutic applications.
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| References | |
| Additional Infomation |
Aberrant tau ligand 1 is a research‑grade compound used exclusively for PROTAC synthesis targeting pathological tau. It is not a drug and has not entered clinical trials or received regulatory approval. The compound has been used to develop PROTAC tau degraders for studying tau‑related neurodegenerative diseases (e.g., Silva et al., eLife, 2019).
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| Molecular Formula |
C14H12N2O2
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|---|---|
| Molecular Weight |
240.26
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| Exact Mass |
240.089
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| CAS # |
1892461-96-9
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| PubChem CID |
116986068
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| Appearance |
Solid powder
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| Density |
1.387±0.06 g/cm3(Predicted)
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| Boiling Point |
529.5±35.0 °C(Predicted)
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
321
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2=C(C=CC(CCC(O)=O)=C2)C2C=NC=CC1=2
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| InChi Key |
FFZYKDATHLINEZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12N2O2/c17-14(18)4-2-9-1-3-10-11-8-15-6-5-12(11)16-13(10)7-9/h1,3,5-8,16H,2,4H2,(H,17,18)
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| Chemical Name |
3-(5H-pyrido[4,3-b]indol-7-yl)propanoic acid
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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) |
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 | 4.1622 mL | 20.8108 mL | 41.6216 mL | |
| 5 mM | 0.8324 mL | 4.1622 mL | 8.3243 mL | |
| 10 mM | 0.4162 mL | 2.0811 mL | 4.1622 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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