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Synonyms | Guanfacine, Tenex, Intuniv | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C9H9Cl2N3O.HCl |
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分子量 | 282.55 | CAS No. | 29110-48-3 | |
Solubility (25°C)* | 体外 | DMSO | 56 mg/mL (198.19 mM) | |
Ethanol | 56 mg/mL (198.19 mM) | |||
Water | 30 mg/mL (106.17 mM) | |||
* <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 | Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect. |
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細胞アッセイ | 細胞株 | LLC-PK1 and LLC-PK1/MDR1 cells |
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濃度 | 5 μM | |
反応時間 | 1 h | |
実験の流れ | Cells (1 mL) are seeded into 24-well plates at a density of 1 × 105 cells/mL. Culture medium is replaced every two days until cells reached confluence. To investigate the potential influence of P-gp on guanfacine transport, intracellular accumulation of guanfacine is measured in LLC-PK1/MDR1 cells and P-gp-negative LLC-PK1 cells. Rhodamine6G, a well-known P-gp substrate, is included as a positive control. After cells reach confluence, the culture medium is replaced by transport buffer for a 30-minute preincubation at 37°C. Transport buffer is then removed and the test compounds (5 μM rhodamine6G, 5 μM guanfacine, or 50 μM guanfacine) are added, and an additional 60-minute incubation period commenced. Next, the solutions are discarded, and the cells are washed three times with ice-cold Dulbecco’s phosphate-buffered saline and solubilized with 1% Triton X-100. Intracellular accumulation of rhodamine6G is measured using a fluorescent microplate reader with a 530 nm excitation and a 580 nm emission wavelength, which is a well established method. Cellular retention of guanfacine is analyzed by the high-performance liquid chromatographic assay described below. The concentrations of rhodamine6G and guanfacine are calculated from their respective standard curves, and standardized with the cellular protein content determined by a Pierce bicinchoninic acid protein kit. |
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動物実験 | 動物モデル | Rats |
投薬量 | 0.075, 0.15, 0.3, and 0.6 mg/kg | |
投与方法 | i.p. |
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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。