GSK-5498A( GSK5498A )

Catalog No. M11016 CAS No. 1253186-49-0

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HPLC

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Product Name

GSK-5498A
Note

Research use only, not for human use.
Brief Description

GSK-5498A is a potent, selective small molecule blocker of Calcium-Release Activated Calcium (CRAC) channel with IC50 of 1 uM.
Description

GSK-5498A is a potent, selective small molecule blocker of Calcium-Release Activated Calcium (CRAC) channel with IC50 of 1 uM; completely inhibits calcium influx through CRAC channels, inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells from multiple human and rat preparations.
In Vitro

GSK-5498A (1 and 10 μM) inhibits calcium influx through CRAC channels in human embryonic kidney cells.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.GSK-5498A (1 nM-10 μM) evokes concentration-dependent inhibition of Cytostim-evoked interferon-γ and IL-5 production in PBMCs.GSK-5498A (1 μM-10 μM) inhibits degranulation of rat tissue-resident mast cells.GSK-5498A (10 nM-10 μM) inhibits mouse and rat T-cell cytokine (IL-2) release.GSK-5498A (0-10 μM) shows high selectivity for CRAC channels over other ion channels, enzymes and G-protein coupled receptors.
In Vivo

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Synonyms

GSK5498A
Pathway

Membrane Transporter/Ion Channel
Target

CRAC Channel
Recptor

CRAC Channel
Research Area

Inflammation/Immunology
Indication

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CAS Number

1253186-49-0
Formula Weight

399.2899
Molecular Formula

C18H11F6N3O
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

C1=CC(=C(C(=C1)F)CN2C=CC(=N2)NC(=O)C3=C(C=CC=C3F)F)C(F)(F)F
Chemical Name

Benzamide, 2,6-difluoro-N-[1-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-3-yl]-

1. Rice LV, et al. Eur J Pharmacol. 2013 Mar 15;704(1-3):49-57. 2. Chen J, et al. J Physiol. 2017 May 15;595(10):3203-3218.

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