[CAS NO. 1253186-49-0]  GSK-5498A

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PRODUCTS SPECIFICATIONS [1253186-49-0]

Catelog
HY-12521
Brand
MCE
CAS
1253186-49-0

DESCRIPTION [1253186-49-0]

Overview

MDL-
Molecular Weight399.29
Molecular FormulaC18H11F6N3O
SMILESO=C(NC1=NN(CC2=C(F)C=CC=C2C(F)(F)F)C=C1)C3=C(F)C=CC=C3F

For research use only. We do not sell to patients.


Summary

GSK-5498A is a selective CARC channel inhibitor ( IC 50 : 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 (pIC 50 : 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] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 250.44 mM )

* "≥" 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
10 mM 0.2504 mL 1.2522 mL 2.5044 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.