Denopamine ((R)-(-)-Denopamine) 是一种有效的，具有口服活性的的选择性 β1-肾上腺素能 (β1-adrenergic) 激动剂。Denopamine 可延长病毒性心肌炎诱发的充血性心力衰竭小鼠模型的存活时间:抑制心脏中肿瘤坏死因子-α 的产生。具有心血管效应。
| Cas No. | 71771-90-9 |
| 别名 | (R)-(-)-Denopamine; TA-064 |
| 分子式 | C18H23NO4 |
| 分子量 | 317.38 |
| 溶解度 | DMSO : 5 mg/mL (15.75 mM; ultrasonic and warming and heat to 60°C) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Denopamine ((R)-(-)-Denopamine) is an orally active, selectiveβ1-adrenergicagonist. Denopamine prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-α production in the heart. Cardiovascular effects[1]. Denopamine (0.1-100 μM) suppresses LPS-induced TNF-α production in a concentration-dependent manner[1]. Cell Viability Assay[1] | Cell Line: | Murine spleen cells | | Concentration: | 0, 0.1, 1, 10, 100 μM | | Incubation Time: | 5 hours | | Result: | Decreased TNF-α levels by 96.9±6.7%, 62.7±6.5%, 53.2±8.8%, and 40.3±1.5% at 0.1, 1, 10 and 100 μmol/L, respectively. |
Denopamine (14 μmol/kg per day; oral administration; for 14 days) significantly improves the survival of the animals, attenuates myocardial lesions, and suppresses TNF-α production in vivo[1].
The plasma concentration of Denopamine is 13.1±1.9 nmol/L at 1 h, 4.3±0.9 nmol/L at 2 h, 1.8±0.5 nmol/L at 3 h, and <0.6 nmol/L at 5 h after its administration. A single 14 μmol/kg dose of denopamine in mice produces a peak level at 1 h[1]. | Animal Model: | Four-week-old inbred male DBA/2 mice[1] | | Dosage: | 14 μmol/kg per day | | Administration: | Oral administration; 14 days | | Result: | Treatment significantly improved the survival of the animals (14 of 25 (56%) treated, vs 5 of 25 (20%) control mice).
At day 14, the survival rate of 57.1% (16 of 28 mice) in the treated group was significantly higher than the 33.3% (10 of 30 mice) survival rate in the control group.
The survival rate from day 6 to day 14 was also significantly improved in the treated group (69.6%; 16 of 23 mice) versus the control group (45.5%; 10 of 22 mice, p < 0.05). |
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