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.
For research use only. We do not sell to patients.
- CAS No.: 1606572-10-4
- Formula: C19H23ClF3N3O3S
- Molecular Weight:465.92
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All P2X Receptor Isoforms
More
Biological Activity
|
P2X2 Receptor |
IL-1β |
NLRP3 |
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.
-
Cell Line:LPS-primed THP-1-derived macrophages
-
Concentration:1, 10, 50, 100 μM
-
Incubation Time:30 min (pre-incubation before 15-20 min BzATP stimulation)
-
Result:Inhibited BzATP-induced IL-1β secretion in LPS-primed THP-1-derived macrophages in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (SD) (male, 200 g, gouty arthritis model via Coderre method)[1]
-
Dosage:40 mg/kg
-
Administration:i.p.; single dose
-
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
-
CAS No. 1606572-10-4
-
Molecular Weight 465.92
-
Formula C19H23ClF3N3O3S
-
SMILES
O=C(C(CC1=CC=CC(C(F)(F)F)=C1)C)NC2=CC=CC(S(=O)(NCCN)=O)=C2.Cl
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Z1456467176 Related Classifications
HY-184711 Related Classifications
Powered by Bioz