GSK-5498A [1253186-49-0]

Cat# HY-12521-1mL

Size : 10mM/1mL

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

GSK-5498A is a selective CARC channel inhibitor (IC50: 1 μM). GSK-5498A inhibits mediators release from mast cells and pro-inflammatory cytokines release from T cells. GSK-5498A can be used in the research of inflammatory disorders[1].

IC50 & Target

CRAC channel[1]

In Vitro

GSK-5498A (1 and 10 μM) inhibits calcium influx through CRAC channels in human embryonic kidney cells[1].
GSK-5498A (1 nM-10 μM) inhibits the thapsigargin-evoked fluorescence signal (pIC50: 6.3) in Jurkat cells, measured using the calcium sensitive dye: Fluo4-AM[1].
GSK-5498A (1 nM-10 μM) evokes concentration-dependent inhibition of Cytostim-evoked interferon-γ and IL-5 production in PBMCs[1].
GSK-5498A (1 μM-10 μM) inhibits degranulation of rat tissue-resident mast cells[1].
GSK-5498A (10 nM-10 μM) inhibits mouse and rat T-cell cytokine (IL-2) release[1].
GSK-5498A (0-10 μM) shows high selectivity for CRAC channels over other ion channels, enzymes and G-protein coupled receptors[1].

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (250.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5044 mL 12.5222 mL 25.0445 mL
5 mM 0.5009 mL 2.5044 mL 5.0089 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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: ≥ 3 mg/mL (7.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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% Corn Oil

    Solubility: ≥ 3 mg/mL (7.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation
References

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