2. Membrane Transporter/Ion Channel NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. P2X Receptor Reactive Oxygen Species (ROS) Interleukin Related
  4. 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.

GSK1370319A

GSK1370319A Chemical Structure

CAS No. : 1001389-31-6

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GSK1370319A Related Antibodies

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Description

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[1].

IC50 & Target[1]

IL-1β

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
474 nM
Compound: 1a; GSK1370319A
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
[PMID: 31525963]
HEK293 IC50
861.8 nM
Compound: 1a; GSK1370319A
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
[PMID: 31525963]
In Vitro

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.

GSK1370319A Related Antibodies

ELISA Assay[1]

Cell Line: differentiated human THP-1 macrophages
Concentration: 10-5 M, 10-6 M
Incubation Time: 2 h, 4 h, 6 h (post LPS and BzATP exposure)
Result: Maintained IL-1β production at basal levels at 2, 4, and 6 h post-stimulation with LPS and BzATP at 10-5 M.

Cell Viability Assay[1]

Cell Line: differentiated human THP-1 macrophages
Concentration: 10-5 M, 10-6 M
Incubation Time: 2 h, 4 h, 6 h (post LPS and BzATP exposure)
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.
In Vivo

GSK1370319A (compound 1a) (2.5 mg/kg; i.p.; daily) reduces the inflammatory index and improves symptoms in a mouse model of DSS-induced acute colitis[1].

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

Animal Model: C57Bl6/J mice (female, 8 weeks old) with DSS-induced acute colitis[1]
Dosage: 2.5 mg/kg
Administration: i.p.; daily; 15 days
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.
Molecular Weight

301.17

Formula

C13H14Cl2N2O2
CAS No.
SMILES

C(NCC1=C(Cl)C=C(Cl)C=C1)(=O)[C@H]2N(C)C(=O)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GSK1370319A Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK1370319A1001389-31-6P2X ReceptorReactive Oxygen Species (ROS)Interleukin RelatedP2XRsILreactive oxygen specieshuman cancer cell linesIL-1βmouse hepatocytesdextran sulfate sodium-induced colitisinflammatory bowel diseasemacrophagehuman P2X7 receptorpro-inflammatory pathwaysmiceInhibitorinhibitorinhibit

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