产品说明书
Fimasartan
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同义名 : | BR-A-657;Kanarb |
| CAS号 : | 247257-48-3 | |
| 货号 : | A349742 | |
| 分子式 : | C27H31N7OS | |
| 纯度 : | 98% | |
| 分子量 : | 501.646 | |
| MDL号 : | MFCD13194795 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(99.67 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Fimasartan (BR-A-657) is an angiotensin receptor II antagonist. Fimasartan displaced angiotensin II (Ang II) from its specific binding sites to AT1 subtype receptors in membrane fractions of HEK-293 cells with an IC50 of 0.16 nM. In conscious rats, Fimasartan (0.01, 0.1, 1 mg/kg; intravenously) dose-dependently antagonized Ang II-induced pressor responses. Fimasartan dose-dependently decreased mean arterial pressure in furosemide-treated rats and renal hypertensive rats. Fimasartan given orally at 1 and 3 mg/kg reduced blood pressure in conscious renal hypertensive rats[2]. In addition, fimasartan down-regulates the expression of the iNOS (inducible nitric oxide synthase) in macrophages via NF-κB (nuclear factor-kappa B) and AP-1 (activator protein-1) inactivation[3]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03649646 | - | Recruiting | September 9, 2020 | Korea, Republic of ... 展开 >> Ajou University Hospital Recruiting Suwon, Korea, Republic of Contact: Seung-Jae Tahk 收起 << | |
| NCT02394392 | - | Completed | - | Korea, Republic of ... 展开 >> Korea university Guro hospital Seoul, Korea, Republic of 收起 << | |
| NCT03254914 | - | Recruiting | September 30, 2019 | Korea, Republic of ... 展开 >> Seoul national university hospital Recruiting Seoul, Korea, Republic of Contact: Hae-young Lee, MD 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.97mL 1.99mL 1.00mL |
19.93mL 3.99mL 1.99mL |
| 参考文献 |
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