| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
TASK-3 (KCNK9) - a two-pore domain potassium channel; TWIK2 - a tandem pore domain weak inward rectifying K+ channel; NLRP3 inflammasome. NPBA is an agonist of TASK-3 and a blocker of TWIK2. TASK-3 is a background potassium channel that regulates resting membrane potential and excitability. TWIK2 is involved in macrophage function and inflammation. NPBA also inhibits NLRP3 inflammasome activation in macrophages.
|
|---|---|
| ln Vitro |
NPBA is a potent and selective agonist of TASK-3 (KCNK9) and a blocker of TWIK2. It significantly inhibits the activation of the NLRP3 inflammasome in macrophages. Detailed in vitro activity data (EC50, IC50) are not provided in the available literature.
|
| ln Vivo |
NPBA suppresses NLRP3 inflammasome activation in macrophages. By modulating potassium channels and inhibiting NLRP3 inflammasome activation, NPBA may have potential applications in inflammatory diseases. In vivo activity data are not provided in the available literature.
|
| Enzyme Assay |
In vitro potassium channel assays are performed using patch-clamp electrophysiology on cells expressing TASK-3 or TWIK2 channels. Cells are treated with varying concentrations of NPBA, and channel currents are measured to determine agonist (TASK-3) or blocker (TWIK2) activity. EC50 or IC50 values are calculated from dose-response curves.
|
| Cell Assay |
Macrophages are treated with NPBA and stimulated with LPS and ATP to activate the NLRP3 inflammasome. IL-1β and IL-18 secretion is measured by ELISA. Caspase-1 activation is assessed by Western blotting or fluorogenic substrate cleavage. The effect of NPBA on potassium channel activity can be confirmed by patch-clamp electrophysiology.
|
| Animal Protocol |
Animal models of inflammatory diseases (e.g., peritonitis, colitis) could be used to assess NPBA's in vivo activity. However, detailed in vivo protocols are not available in the literature. NPBA would be administered via intraperitoneal or oral routes, and inflammation markers would be assessed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of NPBA have not been extensively characterized. Molecular formula: C16H14F3N3O3, molecular weight: 353.30. LogP: 3.6. Appearance: light yellow to green yellow solid powder. Detailed PK data (Cmax, Tmax, AUC, t1/2) are not available in the literature.
|
| Toxicity/Toxicokinetics |
Toxicological data for NPBA are not available. As a potassium channel modulator and NLRP3 inflammasome inhibitor, its toxicity profile is unknown. Standard laboratory safety practices should be followed when handling the compound. It is not intended for human use.
|
| References |
|
| Additional Infomation |
NPBA is a research-grade potassium channel modulator and NLRP3 inflammasome inhibitor. CAS: 524033-40-7. Molecular formula: C16H14F3N3O3, molecular weight: 353.30. It is a potent and selective agonist of TASK-3 (KCNK9) and a blocker of TWIK2. It significantly inhibits NLRP3 inflammasome activation in macrophages. For research use only.
|
| Molecular Formula |
C16H14F3N3O3
|
|---|---|
| Molecular Weight |
353.295874118805
|
| Exact Mass |
353.098
|
| CAS # |
524033-40-7
|
| PubChem CID |
2930995
|
| Appearance |
Light yellow to green yellow solid powder
|
| LogP |
3.6
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
25
|
| Complexity |
462
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C(C=C1)C(=O)NCCNC2=C(C=C(C=C2)[N+](=O)[O-])C(F)(F)F
|
| InChi Key |
LUJDPMMSYZQCHA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H14F3N3O3/c17-16(18,19)13-10-12(22(24)25)6-7-14(13)20-8-9-21-15(23)11-4-2-1-3-5-11/h1-7,10,20H,8-9H2,(H,21,23)
|
| Chemical Name |
N-[2-[4-nitro-2-(trifluoromethyl)anilino]ethyl]benzamide
|
| 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 (In Vitro) |
DMSO :~100 mg/mL (~283.05 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.08 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 and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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 | 2.8305 mL | 14.1523 mL | 28.3046 mL | |
| 5 mM | 0.5661 mL | 2.8305 mL | 5.6609 mL | |
| 10 mM | 0.2830 mL | 1.4152 mL | 2.8305 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
