S-2474
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory agent.
For research use only. We do not sell to patients.
- CAS No.: 158089-95-3
- Formula: C20H31NO3S
- Molecular Weight:365.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
COX-2 11 nM (IC50) |
COX-1 27 μM (IC50) |
5-LO |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
10 μM
Compound: 10b
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In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells
In vitro effect on production of lipopolysaccharide (LPS) -induced IL1-beta in human THP-1 cells
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[PMID: 10821716] |
In Vitro
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s of 11 nM and 27 μM for COX-2 and COX-1[1]. S-2474 prevents neurons from Aβ-induced cell death significantly in a concentration-dependent manner (IC50 =26±12 nM). S-2474 (10 μM) completely inhibits Aβ(25-35)-induced neuronal cell death. S-2474 also shows neuroprotective effects in the Aβ(1-40)-induced neuronal cell death. S-2474 inhibits the PGD2 generation in a concentration dependent manner (IC50=69.8±21.9 nM). S-2474 (10 μM) lowers the elevated level of PGD2 significantly and reduces radicals from Aβ(25-35)-treated neurons[2]. S-2474 significantly prevents neurons from undergoing sPLA2-IIA-induced cell death. S-2474 completely ameliorates sPLA2-IIA-induced apoptotic features such as the condensation of chromatin and the fragmentation of DNA. Moreover, S-2474 significantly inhibits the sPLA2-IIA-induced generation of PGD2. S-2474 inhibits sPLA2-IIA-induced neuronal cell death in a concentration-dependent manner (IC50 = 94 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 158089-95-3
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Molecular Weight 365.53
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Formula C20H31NO3S
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SMILES
OC1=C(C(C)(C)C)C=C(/C=C2CCN(CC)S\2(=O)=O)C=C1C(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
[1]. Yagami T, et al. Effects of S-2474, a novel nonsteroidal anti-inflammatory drug, on amyloid beta protein-induced neuronal cell death. Br J Pharmacol. 2001 Oct;134(3):673-81. [Content Brief]
[2]. Yagami T, et al. S-2474, a novel nonsteroidal anti-inflammatory drug, rescues cortical neurons from human group IIA secretory phospholipase A(2)-induced apoptosis. Neuropharmacology. 2005 Aug;49(2):174-84. Epub 2005 Apr 1. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)