INF39 [866028-26-4]

Referencia HY-101868-5mg

embalaje : 5mg

Marca : MedChemExpress

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Teléfono : +1 850 650 7790

Descripciòn

INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.

IC50 & Target

NLRP3

 

In Vitro

INF39 is able to significantly inhibit ATP- and nigericin-induced IL-1β release at 10 μM. INF39 reduces caspase-1 activation and pyroptosis in the macrophages. INF39 can block not only NLRP3 activation but also the NF-κB pathway. INF39 potentially reacts with Cys-SH residues in the active site of cysteine protease caspase-1, but does not directly target caspase-1 activity. INF39 is able to reduce the steady state (or basal) BRET signal of NLRP3 without affecting the viability of cells, meaning that it can interfere with the basal NLRP3 conformation. INF39 does not block the initial conformational changes suffered by NLRP3 upon sensing the decrease of intracellular K+; however, it affects a second step of NLRP3 conformational change that could be related with the ATPase activity of the receptor and be independent of the decrease of intracellular K+. INF39 reaches the intestinal epithelium without undergoing chemical modifications. After absorption into epithelial cells, it is likely to act locally at the mucosal epithelial level[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (445.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4508 mL 22.2539 mL 44.5077 mL
5 mM 0.8902 mL 4.4508 mL 8.9015 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (11.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (11.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Pureza y Documentación
Referencias

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