2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. GSK1370319A

GSK1370319A (compound 1a) 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.

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GSK1370319A

GSK1370319A Chemical Structure

CAS No. : 1001389-31-6

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GSK1370319A Related Antibodies

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Description

GSK1370319A (compound 1a) 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].

In Vitro

GSK1370319A (compound 1a) (10-5 M; 15 min pre-incubation, 1 h post BzATP addition) fully inhibits human P2X7 receptor activation in human P2X7-expressing HEK293 cells with an IC50 of 474.0 nM[1].
GSK1370319A (1 h) binds to human P2X7 receptors in human P2X7-expressing HEK293 cell membranes with a Ki of 176 nM and an IC50 of 861.8 nM[1].
GSK1370319A (10-5 M; 0-5 h post LPS and BzATP exposure) potently inhibits LPS- and BzATP-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].
GSK1370319A (40 min) exhibits high metabolic stability, with a half-life of 619 min, an intrinsic clearance of 3.6 μL/min/mg, and only 5.1% metabolization by mouse hepatocytes after 40 min[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 by 50% and improves clinical 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 (female, 8 weeks old)[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 ReceptorP2XRsreactive oxygen specieshuman cancer cell linesIL-1βmouse hepatocytesdextran sulfate sodium-induced colitisinflammatory bowel diseasemacrophagehuman P2X7 receptorpro-inflammatory pathwaysmiceInhibitorinhibitorinhibit

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