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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1606572-10-4
- 分子式: C19H23ClF3N3O3S
- 分子量:465.92
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保管条件:
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]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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P2X Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
P2X2 Receptor |
IL-1β |
NLRP3 |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 1606572-10-4
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分子量 465.92
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Z1456467176 関連分類
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