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Darusentan (Lu-135252) 是内皮素受体 A (ET-A) 受体选择性拮抗剂,能够作用于 ET-A 受体(Ki:1.4 nM)及ET-B 受体(Ki:184 nM),对 ETA 受体的选择性大于 ETB 受体的100以上。它在大鼠主动脉血管平滑肌细胞膜中竞争结合放射性标记的内皮素(Ki:13 nM)。
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Darusentan (Lu-135252) 是内皮素受体 A (ET-A) 受体选择性拮抗剂,能够作用于 ET-A 受体(Ki:1.4 nM)及ET-B 受体(Ki:184 nM),对 ETA 受体的选择性大于 ETB 受体的100以上。它在大鼠主动脉血管平滑肌细胞膜中竞争结合放射性标记的内皮素(Ki:13 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 397 | 现货 | |
2 mg | ¥ 595 | 现货 | |
5 mg | ¥ 996 | 现货 | |
10 mg | ¥ 1,830 | 现货 | |
25 mg | ¥ 3,120 | 现货 | |
50 mg | ¥ 4,590 | 现货 | |
100 mg | ¥ 6,530 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 997 | 现货 |
产品描述 | Darusentan (Lu-135252) is a potent inhibitor of endothelin signaling and function in both large and small arteries |
体外活性 | Darusentan 抑制与促收缩活动有关的内皮素诱导信号,并且是大、小动脉血管收缩强效抑制剂。 |
细胞实验 | Briefly, isolated rat aortic smooth muscle cells were incubated overnight in complete media in a 96-well microplate at a density of 50 000 cells/well. The next day, cells were starved for 24 h in 0% serum conditions. Following starvation, medium was removed and cells were dosed with 20 μL of increasing concentrations of darusentan (0, 0.001, 0.01, 0.1, 1, and 10 μmol/L) made in stimulation buffer containing 50 mmol/L LiCl. Cells were incubated at 37 °C, 5% CO2 for 30 min before the addition of 20 μL of ET-1 in dose-response fashion. Cells were incubated in the presence or absence of darusentan and ET-1 at 37 °C, 5% CO2 for 60 min. Following this incubation, cells were lysed using 20 μL of 2.5% lysis solution for 30 min and lysates were transferred to a 96-well microplate pre-coated with goat anti-mouse IgG. After transfer into the ELISA plate, kit-supplied IP1-horseradish peroxidase (HRP) conjugate and anti-IP1 mAb were added to the lysates. Assays were incubated for 3 h at room temperature on a platform shaker. Assay plates were then washed 6 times with 1× ELISA wash solution (250 μL/well) before the addition of HRP substrate TMB (3, 3', 5, 5'-tetramethylbenzidine). After 20 min, the reaction was stopped and the optical density (OD) was measured at 450 nm with a correction of 620 nm. Measurements were performed in triplicate. |
别名 | 达卢生坦, Lu-135252 |
分子量 | 410.43 |
分子式 | C22H22N2O6 |
CAS No. | 171714-84-4 |
Smiles | COc1cc(OC)nc(O[C@H](C(O)=O)C(OC)(c2ccccc2)c2ccccc2)n1 |
密度 | 1.268g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 125 mg/mL (304.57 mM) H2O: Insoluble | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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