Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
Targets |
Kd: 160 μM (Aβ1-42)[1]. Kd: 337 μM (tau)[1]
|
---|---|
ln Vitro |
The tau aggregation foci are greatly reduced by Aβ/tau aggregation-IN-1 (1 μM; 24 hours; HEK-293 T cells)[1]. Aβ/tau aggregation-IN-1 efficiently inhibits tau aggregation by 71.2%–101.8% and Aβ1–42 aggregation by 84.7%–99.5% when the quinolone ring is N-methylated. Aβ/tau aggregation-IN-1 prevents the production of β-sheets, which in turn prevents self-induced Aβ1-42 aggregation. Aβ/tau aggregation-IN-1 demonstrates specific binding properties with tau and Aβ1-42. Aβ/tau aggregation-IN-1 with Aβ1-42 has a KD value of 160 μM. Aβ/tau aggregation-IN-1 with tau has a KD value of 337 μM. Through noncovalent interactions, tau and Aβ1-42 are interacting with Aβ/tau aggregation-IN-1[1].
|
Cell Assay |
Immunofluorescence[1]
Cell Types: HEK-293 T cells Tested Concentrations: 1 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically declined the tau aggregation foci. |
References |
[1]. Lv P, et al. Synthesis and evaluation of 1,2,3,4-tetrahydro-1-acridone analogues as potential dual inhibitors for amyloid-beta and tau aggregation. Bioorg Med Chem. 2018;26(16):4693-4705.
|
Molecular Formula |
C25H21IN2O
|
---|---|
Molecular Weight |
492.35
|
CAS # |
2252162-81-3
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C[N+]1C2=CC=CC=C2C(N)=C2C(/C(=C/C3C4C(C=CC=3)=CC=CC=4)/CCC=12)=O.[I-]
|
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 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)
|
Solubility (In Vitro) |
DMSO: 33.33 mg/mL (67.70 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.03 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 mg/mL (2.03 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 10.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0311 mL | 10.1554 mL | 20.3108 mL | |
5 mM | 0.4062 mL | 2.0311 mL | 4.0622 mL | |
10 mM | 0.2031 mL | 1.0155 mL | 2.0311 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.