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NCI 126224

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Catalog No. T83895Cas No. 65974-52-9
Alias NCI-126224, NCI126224

NCI 126224 is a Toll-like receptor 4 (TLR4) antagonist that selectively inhibits nitric oxide production induced by the TLR4 agonist LPS in RAW 264.7 macrophages (IC50 = 0.31 µM), while exhibiting weaker effects against the TLR7/8 agonist R-848, TLR1/2 agonist Pam3CSK4, and TLR3 agonist poly(I:C). NCI 126224 also inhibits FSL-1-induced NO production at 0.6 µM and suppresses LPS-induced NF-κB activity in BV-2 glial cells, while reducing IL-1β and TNF-α levels in RAW 264.7 cells (IC50s of 5.92 and 1.54 µM, respectively). 0.42, and 1.54 µM, respectively), demonstrating its significant value in studies of inflammatory and innate immune signaling pathways.

NCI 126224

NCI 126224

😃Good
Catalog No. T83895Alias NCI-126224, NCI126224Cas No. 65974-52-9
NCI 126224 is a Toll-like receptor 4 (TLR4) antagonist that selectively inhibits nitric oxide production induced by the TLR4 agonist LPS in RAW 264.7 macrophages (IC50 = 0.31 µM), while exhibiting weaker effects against the TLR7/8 agonist R-848, TLR1/2 agonist Pam3CSK4, and TLR3 agonist poly(I:C). NCI 126224 also inhibits FSL-1-induced NO production at 0.6 µM and suppresses LPS-induced NF-κB activity in BV-2 glial cells, while reducing IL-1β and TNF-α levels in RAW 264.7 cells (IC50s of 5.92 and 1.54 µM, respectively). 0.42, and 1.54 µM, respectively), demonstrating its significant value in studies of inflammatory and innate immune signaling pathways.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$12735 days35 days
5 mg$51935 days35 days
10 mg$84535 days35 days
25 mg$1,60035 days35 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
NCI 126224 is a Toll-like receptor 4 (TLR4) antagonist that selectively inhibits nitric oxide production induced by the TLR4 agonist LPS in RAW 264.7 macrophages (IC50 = 0.31 µM), while exhibiting weaker effects against the TLR7/8 agonist R-848, TLR1/2 agonist Pam3CSK4, and TLR3 agonist poly(I:C). NCI 126224 also inhibits FSL-1-induced NO production at 0.6 µM and suppresses LPS-induced NF-κB activity in BV-2 glial cells, while reducing IL-1β and TNF-α levels in RAW 264.7 cells (IC50s of 5.92 and 1.54 µM, respectively). 0.42, and 1.54 µM, respectively), demonstrating its significant value in studies of inflammatory and innate immune signaling pathways.
In vivo
Structurally related arylidene malonate derivatives developed from the NCI 126224 scaffold exhibit anti-inflammatory activity in vivo. In a mouse model of xylene-induced ear edema, optimized analogues such as Compound 3e reduced swelling and inflammation in a dose-dependent manner [1].
SynonymsNCI-126224, NCI126224
Chemical Properties
Molecular Weight265.2
FormulaC12H11NO6
Cas No.65974-52-9
SmilesCOC(/C(C(OC)=O)=C/C1=C(C=CC=C1)[N+]([O-])=O)=O
Storage & Solubility Information
Storagekeep away from moisture | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: Soluble
Methanol: Soluble
Chloroform: Soluble
DMSO: 100 mg/mL (377.07 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.7707 mL18.8537 mL37.7074 mL188.5370 mL
5 mM0.7541 mL3.7707 mL7.5415 mL37.7074 mL
10 mM0.3771 mL1.8854 mL3.7707 mL18.8537 mL
20 mM0.1885 mL0.9427 mL1.8854 mL9.4268 mL
50 mM0.0754 mL0.3771 mL0.7541 mL3.7707 mL
100 mM0.0377 mL0.1885 mL0.3771 mL1.8854 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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