Z1456467176
Z1456467176 is an allosteric inhibitor of P2X7R. Z1456467176 binds to P2X7R, prevents ATP-induced channel opening and receptor activation, and blocks ATP-induced activation of the NLRP3-caspase-1-IL-1β pathway. Z1456467176 inhibits ATP-induced P2X7R pore formation in macrophages, as well as IL-1β secretion induced by ATP or BzATP. Z1456467176 alleviates gouty joint inflammation in rats. Z1456467176 can be used for the research of gouty arthritis.
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- CAS No.: 1606572-10-4
- Formule: C19H23ClF3N3O3S
- Masse moléculaire:465.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
P2X2 Receptor |
IL-1β |
NLRP3 |
In Vitro
Z1456467176 potently inhibits ATP-induced P2X7R pore formation in HEK-293T cells overexpressing hP2X7R with an IC50 of 3.416 μM[1].
Z1456467176 (1-100 μM; 30 min pre-incubation before 15-20 min BzATP stimulation) dose-dependently inhibits BzATP-induced IL-1β secretion in LPS-primed THP-1-derived macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-primed THP-1-derived macrophages
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Concentration:1, 10, 50, 100 μM
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Incubation Time:30 min (pre-incubation before 15-20 min BzATP stimulation)
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Result:Inhibited BzATP-induced IL-1β secretion in LPS-primed THP-1-derived macrophages in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male, 200 g, gouty arthritis model via Coderre method)[1]
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Dosage:40 mg/kg
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Administration:i.p.; single dose
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Result:Reduced ankle circumference and swelling index versus MSU monotherapy group.
Decreased intra-tissue inflammatory cell density from ~53 to ~32 cells per field.
Suppressed tissue MPO activity from ~18 U/g to ~13 U/g tissue.
Diminished serum IL-1β concentration from ~250 pg/mL to ~150 pg/mL.
Downregulated relative IL-1β transcriptional level from ~2.8 to ~1.5.
Blocked MSU-triggered upregulation of NLRP3, caspase-1 (p20) and IL-1β protein in joint and synovial tissues.
Exerted no adverse impact on hepatic (AST, ALT) and renal (BUN, Cr) biochemical markers.
Chemical Information
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CAS No. 1606572-10-4
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Masse moléculaire 465.92
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Formule C19H23ClF3N3O3S
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SMILES
O=C(C(CC1=CC=CC(C(F)(F)F)=C1)C)NC2=CC=CC(S(=O)(NCCN)=O)=C2.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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