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Synonyms | N/A | Storage (From the date of receipt) |
3 years-20°C powder | |
化学式 | C19H17NO5S |
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分子量 | 371.41 | CAS No. | 1133819-87-0 | |
Solubility (25°C)* | 体外 | DMSO | 82 mg/mL (220.78 mM) | |
Water | Insoluble | |||
Ethanol | 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 | Azemiglitazone (MSDC-0602) is a direct mitochondrial pyruvate carrier (MPC) inhibitor that modulates central carbon metabolism in mice and humans. |
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in vitro | Azemiglitazone (MSDC-0602) is a modified hiazolidinediones (TZDP) with alterations in the carbon backbone that limit the ability to bind PPARγ, with the IC50 for PPARγ of 18.25 μM. Azemiglitazone (MSDC-0602) also shows the affinity for mitochondrial binding, with the IC50 of 1.38 μM. Using a Gal4-PPARγ construct containing the ligand binding domain of mouse PPARγ, MSDC-0602 only minimally activates Gal4-PPARγ in HepG2 cells even at a concentration of 50 μM.<sup><a class="sref" href="#s_ref">[1]</a></sup><sup><a class="sref" href="#s_ref">[2]</a></sup> |
in vivo | Azemiglitazone (MSDC-0602) corrects plasma glucose, nonesterified fatty acids, triglycerides, cholesterol, and insulin concentrations, which are elevated in ob/ob mice compared with lean controls. Treatment with Azemiglitazone (MSDC-0602) also significantly improved glucose and insulin tolerance in ob/ob mice.<sup><a class="sref" href="#s_ref">[2]</a></sup> |
キナーゼアッセイ | PPAR Binding Assays | |
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TZD binding to the ligand binding domain of PPARγ was assessed in a LanthaScreen TMTR-FRET competitive binding assay performed according the protocol of the manufacturer (Invitrogen). IC 50 values for the PPARγ LanthaScreen were determined using Gen5 software (BioTek Instruments, Inc.). R2 values for individual IC50 values ranged from 0.983 to 0.999 based on three separate assays for each compound. | ||
細胞アッセイ | 細胞株 | HepG2 hepatoma cells |
濃度 | 0.5 nM, 5 nM, 50 nM, 0.5 μM, 5 μM and 50μM | |
反応時間 | 48 h | |
実験の流れ | HepG2 hepatoma cells were co-transfected by calcium phosphate coprecipitation with expression vectors for Gal4-PPARγ (ligand binding domain only) or Gal4-PPARα, heterologous firefly luciferase reporter construct driven by five copies of a Gal4 response element, and SV40-driven renilla luciferase reporter construct. Transfected cells were treated with PPARγ agonists (rosiglitazone and pioglitazone), PPARα agonist (GW7647), or MSDC-0602 for 24 h. Cell lysate firefly and renilla luciferase activity was assessed 48 h later by using the Dual-Glo kit. Firefly luciferase activity was corrected for renilla luciferase activity, and DMSO (vehicle) values were normalized to 1.0. |
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動物実験 | 動物モデル | Liver-specific (LS)-PPARγ-/- mice |
投薬量 | 30 mg/kg/day | |
投与方法 | p.o. |
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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。