GSK1370319A
GSK1370319A is a human P2X7 receptor inhibitor with an IC50 of 474 nM and a Ki of 176 nM. GSK1370319A inhibits the production of IL-1β, reduces the generation of reactive oxygen species (ROS), and increases the survival rate of macrophages. GSK1370319A can be used for the research of inflammatory bowel disease.
For research use only. We do not sell to patients.
- CAS No.: 1001389-31-6
- Formula: C13H14Cl2N2O2
- Molecular Weight:301.17
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All P2X Receptor Isoforms
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Biological Activity
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IL-1β |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
474 nM
Compound: 1a; GSK1370319A
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Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome
Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome
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[PMID: 31525963] |
| HEK293 | IC50 |
861.8 nM
Compound: 1a; GSK1370319A
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Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method
Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method
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[PMID: 31525963] |
GSK1370319A (compound 1a) (10-5 M; 0-5 h post LPS and BzATP exposure) potently inhibits LPS (HY-D1056)- and BzATP (HY-136254)-induced ROS production in differentiated human THP-1 macrophages[1].
GSK1370319A (10-6-10-5 M; 2-6 h post LPS and BzATP exposure) protects differentiated human THP-1 macrophages from LPS- and BzATP-induced cell death at 2 and 4 h, but not at 6 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:differentiated human THP-1 macrophages
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Concentration:10-5 M, 10-6 M
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Incubation Time:2 h, 4 h, 6 h (post LPS and BzATP exposure)
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Result:Maintained IL-1β production at basal levels at 2, 4, and 6 h post-stimulation with LPS and BzATP at 10-5 M.
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Cell Line:differentiated human THP-1 macrophages
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Concentration:10-5 M, 10-6 M
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Incubation Time:2 h, 4 h, 6 h (post LPS and BzATP exposure)
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Result:Increased macrophage survival relative to LPS- and BzATP-treated controls at 2 and 4 h, but the protective effect was lost by 6 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl6/J mice (female, 8 weeks old) with DSS-induced acute colitis[1]
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Dosage:2.5 mg/kg
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Administration:i.p.; daily; 15 days
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Result:Reduced weight loss, improved stool consistency, and decreased rectal bleeding compared to untreated controls.
Reduced severity and extent of inflammation, decreased crypt damage, and a smaller percentage of tissue affected by inflammation, resulting in a 50% reduction in the inflammatory index relative to untreated mice.
Chemical Information
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CAS No. 1001389-31-6
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Molecular Weight 301.17
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Formula C13H14Cl2N2O2
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SMILES
C(NCC1=C(Cl)C=C(Cl)C=C1)(=O)[C@H]2N(C)C(=O)CC2
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK1370319A Related Classifications
HY-165557 Related Classifications
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