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
- 화학식: C19H23ClF3N3O3S
- 분자량:465.92
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All P2X Receptor Isoforms
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Biological Activity
제품 설명
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. Further protocols information, click here.
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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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분자량 465.92
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Pyroptosis Solutions
Pyroptosis is a lytic inflammatory cell-death pathway executed by gasdermin pores, most classically through inflammasome-mediated activation of caspase-1, cleavage of gasdermin D, membrane pore formation, LDH release, and secretion of IL-1β and IL-18. The canonical pathway is commonly modeled by priming cells with an inflammatory signal such as LPS to induce pro-IL-1β and inflammasome components, followed by an activation signal such as ATP or nigericin to activate NLRP3, ASC speck formation, caspase-1 cleavage, GSDMD cleavage, cytokine release, and pyroptotic membrane rupture. The non-canonical pathway is triggered when cytosolic LPS activates mouse caspase-11 or human caspase-4/5, leading to GSDMD cleavage and pyroptosis, and this can secondarily activate NLRP3-dependent IL-1β release. Pyroptosis is linked to inflammatory injury, infection, cancer, liver disease, ocular disease, placental inflammation, and other disease phenotypes, but unresolved questions include which gasdermin fam
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)