GSK-5498A
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 1253186-49-0
- Formula: C18H11F6N3O
- Molecular Weight:399.29
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GSK-5498A
More
Biological Activity
CRAC channel[1]
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.
Chemical Information
-
CAS No. 1253186-49-0
-
Appearance Solid
-
Molecular Weight 399.29
-
Formula C18H11F6N3O
-
Color White to off-white
-
SMILES
O=C(NC1=NN(CC2=C(F)C=CC=C2C(F)(F)F)C=C1)C3=C(F)C=CC=C3F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
2020 Oct 30;11(1):5489. PMID: 33127885 -
Adv Sci (Weinh)
Extracellular Vesicles Derived from Human Umbilical Cord Mesenchymal Stem Cells Protect Liver Ischemia/Reperfusion Injury by Reducing CD154 Expression on CD4+ T Cells via CCT2. [Abstract]2020 Aug 20;7(18):1903746. PMID: 32999825 -
J Physiol
Store-operated calcium entry is required for sustained contraction and Ca2+ oscillations of airway smooth muscle. [Abstract]2017 May 15;595(10):3203-3218. PMID: 27396568
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5044 mL | 12.5222 mL | 25.0445 mL | 62.6111 mL |
| 5 mM | 0.5009 mL | 2.5044 mL | 5.0089 mL | 12.5222 mL | |
| 10 mM | 0.2504 mL | 1.2522 mL | 2.5044 mL | 6.2611 mL | |
| 15 mM | 0.1670 mL | 0.8348 mL | 1.6696 mL | 4.1741 mL | |
| 20 mM | 0.1252 mL | 0.6261 mL | 1.2522 mL | 3.1306 mL | |
| 25 mM | 0.1002 mL | 0.5009 mL | 1.0018 mL | 2.5044 mL | |
| 30 mM | 0.0835 mL | 0.4174 mL | 0.8348 mL | 2.0870 mL | |
| 40 mM | 0.0626 mL | 0.3131 mL | 0.6261 mL | 1.5653 mL | |
| 50 mM | 0.0501 mL | 0.2504 mL | 0.5009 mL | 1.2522 mL | |
| 60 mM | 0.0417 mL | 0.2087 mL | 0.4174 mL | 1.0435 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3131 mL | 0.7826 mL | |
| 100 mM | 0.0250 mL | 0.1252 mL | 0.2504 mL | 0.6261 mL |