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Tau tracer 2 (Pl-2620)

Cat No.:V35219 Purity: ≥98%
Tau tracer 2 (Pl-2620) is a Tau tracer used for imaging Tau protein aggregates.
Tau tracer 2 (Pl-2620)
Tau tracer 2 (Pl-2620) Chemical Structure CAS No.: 2173361-80-1
Product category: Microtubule(Tubulin)
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
Tau tracer 2 (Pl-2620) is a Tau tracer used for imaging Tau protein aggregates. Tau tracer 2 may be utilized to diagnose neurodegenerative diseases.
Tau tracer 2 (PI-2620) (CAS#: 2173361-80-1) is a specific imaging agent designed to detect and visualize Tau protein aggregates. It is primarily used for diagnosing neurodegenerative diseases, including Alzheimer's disease and other tauopathies, through Positron Emission Tomography (PET) imaging. Tau tracer 2 is a small molecule that binds to Tau aggregates with high affinity and selectivity.
Biological Activity I Assay Protocols (From Reference)
Targets
Tau tracer 2 targets Tau protein aggregates, which are a hallmark of several neurodegenerative diseases, including Alzheimer's disease. It binds to these aggregates with high affinity and specificity, allowing for their detection and visualization using PET imaging. This makes it a valuable tool for diagnosing tauopathies and monitoring disease progression.
ln Vitro
Using Positron Emission Tomography (PET) imaging, Tau tracer 2 (compound F-3a) can be used to selectively detect Tau aggregate-associated illnesses and abnormalities, such as Alzheimer's disease and other tauopathies[1].
In vitro, Tau tracer 2 demonstrates high binding affinity and selectivity for Tau protein aggregates. Its ability to bind to Tau aggregates is assessed using binding assays with synthetic Tau fibrils or brain homogenates from tauopathy patients. The compound shows minimal binding to amyloid-beta plaques, indicating good selectivity for Tau over other pathological protein aggregates.
ln Vivo
In vivo, Tau tracer 2 (compound F-3a) can be used to selectively detect Tau aggregate-associated illnesses and abnormalities in living subjects using PET imaging. It has been evaluated in preclinical and clinical studies for its ability to image Tau pathology in the brain. The tracer shows good brain penetration and specific binding to Tau aggregates, making it a promising diagnostic tool.
Enzyme Assay
The in vitro binding assay for Tau tracer 2 typically involves measuring its affinity for Tau protein aggregates. This is done using radioligand binding assays with synthetic Tau fibrils or brain tissue homogenates. The compound's selectivity for Tau over other proteins, such as amyloid-beta, is also assessed. These assays are crucial for confirming its specificity.
Cell Assay
Cellular assays for Tau tracer 2 are not typically performed, as its primary application is as an imaging agent. Instead, binding studies are conducted using Tau protein aggregates in cell-free systems or brain tissue. The compound's ability to cross the blood-brain barrier is assessed using in vitro models of the blood-brain barrier.
Animal Protocol
In vivo animal protocols for Tau tracer 2 involve intravenous administration of the radiolabeled compound to animal models of tauopathy, such as transgenic mice expressing human Tau. PET imaging is performed to visualize Tau aggregates in the brain. The tracer's biodistribution and specificity are evaluated by ex vivo autoradiography and brain homogenate analysis.
ADME/Pharmacokinetics
Pharmacokinetic (PK) properties of Tau tracer 2 are typical of small-molecule PET tracers. It is designed to have good brain penetration and rapid clearance from non-target tissues. The compound is administered intravenously, and its distribution is assessed by PET imaging. Its half-life and metabolic stability are optimized for imaging applications.
Toxicity/Toxicokinetics
Toxicity data for Tau tracer 2 are limited. As an imaging agent, it is administered at sub-pharmacological doses, minimizing the risk of toxicity. Standard toxicological assessments have been conducted to support its use in clinical PET imaging. The compound is intended for research and diagnostic use only.
References

[1]. Compounds for imaging tau protein aggregates. WO2018015549A1.

Additional Infomation
Tau tracer 2 (PI-2620) is a PET imaging agent for Tau protein aggregates. It is used for diagnosing Alzheimer's disease and other tauopathies. The tracer has been evaluated in clinical trials for imaging Tau pathology in the brain. It is not approved for therapeutic use and is intended for research and diagnostic purposes.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H9FN4
Molecular Weight
264.2572
Exact Mass
264.081
CAS #
2173361-80-1
Related CAS #
2173361-80-1 (F19);2173353-61-0 (F18);
PubChem CID
134202705
Appearance
Off-white to light yellow solid powder
LogP
2.6
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
1
Heavy Atom Count
20
Complexity
353
Defined Atom Stereocenter Count
0
SMILES
FC1C([H])=C(C([H])=C([H])N=1)C1C([H])=C([H])C2=C(N=1)N([H])C1C([H])=C([H])N=C([H])C2=1
InChi Key
JUPWIBZGGFVBCU-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H9FN4/c16-14-7-9(3-6-18-14)12-2-1-10-11-8-17-5-4-13(11)20-15(10)19-12/h1-8H,(H,19,20)
Chemical Name
11-(2-fluoropyridin-4-yl)-4,8,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaene
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 16.67 mg/mL (63.08 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.32 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 16.7 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: ≥ 1.67 mg/mL (6.32 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 16.7 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.

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Solubility in Formulation 3: ≥ 1.67 mg/mL (6.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.7842 mL 18.9208 mL 37.8415 mL
5 mM 0.7568 mL 3.7842 mL 7.5683 mL
10 mM 0.3784 mL 1.8921 mL 3.7842 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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