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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C30H27BrN4O3 |
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分子量 | 571.46 | CAS No. | 2100284-59-9 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (174.99 mM) | |
Ethanol | 100 mg/mL (174.99 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | AZ3451 is a potent antagonist of protease-activated receptor 2 (PAR2) that binds to a remote allosteric site outside the helical bundle with IC50 of 23 nM. |
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in vitro | AZ3451 is a PAR2 antagonist that plays a part in inflammation response, apoptosis, autophagy and cellular senescence during Osteoarthritis (OA). AZ3451 prevents the IL-1β-induced inflammation response, cartilage degradation and premature senescence in chondrocytes. AZ3451 attenuates chondrocytes apoptosis by activating autophagy in vitro. The P38/MAPK, NF-κB and PI3K/AKT/mTOR pathways are involved in the protective effect of AZ3451.[2] |
in vivo | Intra-articular injection of AZ3451 can ameliorate the surgery induced cartilage degradation in rat Osteoarthritis (OA) model.[2] |
細胞アッセイ | 細胞株 | chondrocytes |
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濃度 | 10 μM | |
反応時間 | 48 h | |
実験の流れ | Primary rat chondrocytes are derived from the knee joint cartilage tissue of 1-week-old Sprague–Dawley rats. Cartilage pieces are sequential digested with 0.2% trypsin and 0.25% collagenase II dissolved in Dulbecco’s Modified Eagle Medium (DMEM) culture medium. The released chondrocytes are collected and cultured in DMEM supplemented with 10% fetal bovine serum (FBS), 100 units/ml penicillin and 100 μg/ml streptomycin. Up to approximately 80% confluences, cells are treated with 10 μM AZ3451 in the presence or absence of 10 ng/mL IL-1β. Passages 1–3 chondrocytes are used in our experiment to avoid the phenotype loss. |
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動物実験 | 動物モデル | male 8-week-old Sprague–Dawley rats |
投薬量 | 100 μl (50 μg/ml) | |
投与方法 | intra-articular injection |
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長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。