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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | ||||||||
化学式 | C27H33N5O4S |
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分子量 | 523.65 | CAS No. | 2097381-85-4 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (190.96 mM) | ||||||||
Ethanol | 100 mg/mL (190.96 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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 | VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology. |
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in vitro | VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC.[2] |
in vivo | VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC.[2] |
細胞アッセイ | 細胞株 | rFb cells, hUVEC cells |
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濃度 | 10 μM, 30 μM, 100 μM, 200 μM | |
反応時間 | 48 h | |
実験の流れ | The rFb are trypsinised and placed in flat-bottomed 96-well plates at an initial density of 5000 cells per well. After 24 h of incubation, the medium is changed to VH298-containing medium at different dosages (0 μM, 10 μM, 30 μM, 100 μM, and 200 μM). rFb are incubated at 37°C for 48 h. The proliferation is determined by the Cell Counting Kit-8 (CCK-8) assay. After incubation, rFb are treated with the CCK-8 solution at a final concentration of 10% for 2 h at 37°C, followed by measurement of absorbance at 450nm using a microplate reader. |
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動物実験 | 動物モデル | Sprague-Dawley rats intraperitoneal injected of streptozotocin at 65 mg/kg |
投薬量 | 30 μM VH298 in PBS (100 microlitres) | |
投与方法 | local injection |
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Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity [ Eur J Med Chem, 2024, 268:116202] | PubMed: 38394929 |
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。