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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Store at 2-8℃，2 years
- 保质期：
Store at 2-8℃，2 years
- 英文名：
Aliskiren
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
173334-57-1
- 规格：
25mg/10mg/5mg/1mg/50mg
| 规格： | 25mg | 产品价格： | ￥1555.2 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥981.0 |
| 规格： | 5mg | 产品价格： | ￥648.0 |
| 规格： | 1mg | 产品价格： | ￥282.6 |
| 规格： | 50mg | 产品价格： | ￥2151.0 |
是一种肾素抑制剂，具有降压活性。
| 基本信息 | |
| CAS | No.173334-57-1 |
| 中文名称 | 阿利克仑 |
| 英文名称 | Aliskiren |
| 别名 | ;CGP60536;CGP60536B;Rasilez;SPP100;Tekturna; |
| 分子式 | C30H53N3O6 |
| 分子量 | 551.76 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | Liquid |
| 储存条件 | Store at 2-8℃，2 years |
| EC | EINECS 605-672-4 |
| MDL | MFCD09839018 |
| SMILES | COCCCOC1=CC(C[C@@H](C[C@@H]([C@H](C[C@H](C(NCC(C)(C(N)=O)C)=O)C(C)C)O)N)C(C)C)=CC=C1OC |
| 靶点 | Renin |
| 通路 | Endocrinology & Hormones |
| 背景说明 | 是一种肾素抑制剂,具有降压活性。 |
| 生物活性 | Aliskiren is the fourth class of pharmacological agents that modify the function of RAAS. It is an octanamide, is the first known representative of a new class of completely nonpeptide, low-molecular-weight, orally active transition-state renin inhibitors. [1] |
| In Vitro | Aliskiren has good water solubility and low lipophilicity，and is resistant to biodegradation by peptidases in the intestine，blood circulation，and the liver. Aliskiren has 10，000-fold higher affinity for renin than for other aspartic peptidases[1]. |
| 细胞实验 | In short-term studies，Aliskiren is effective in lowering blood pressure either alone or in combination with valsartan and hydrochlorothiazide，and had a low incidence of serious adverse effects. Aliskiren has a half-life of approximately 40 h，making it suitable for once-daily dosing，with less potential for loss of efficacy between doses than shorter acting agents. Aliskiren exhibits oral bioavailability due to its low molecular weight(609.8 Da)and nonpeptide structure，making it more resistant to gastrointestinal enzyme disintegration. However，it is still poorly absorbed(oral bioavailability，～2.5%). Aliskiren is 50% protein bound，and the apparent volume of distribution is 135 L. Aliskiren is slightly metabolized in humans(about 20%)and is approximately 50% metabolized in rodents. Aliskiren effectively reduces functional plasma renin activity by binding to renin with high affinity，preventing it from converting angiotensinogen to angiotensin I. The inhibition of renin by aliskiren is associated with a reduction in circulating levels of angiotensin I and II，with a resultant increase in plasma renin concentration and inhibit activation of mitogen-activated protein kinases ERK1(p44)and ERK2(p42). It prevents hypertrophy and proliferation. Aliskiren is well tolerated，with the most common adverse events reported as headache，dizziness，and fatigue[1]. |
| 数据来源文献 | [1] Pranay Wal， et al. J Pharm Bioallied Sci. 2011， 3(2): 189–193. |
| 单位 | 瓶 |
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文献和实验2F+DwTquooTcizAj6Sh40arj1e+iWJ2ispgsbT801bWi9OaaVDQ0u7N9Rf22Q7je3ypEkT/aXtAx/4gHh20RbetchuWXizve3YY/3L0LGHHqt8Cva+97zf/vEfvyYb4imWXpTxLz8m4rvgjodswc3X26Xnn2o3LbjZPv/Fv5GGuGa33/ZzO2n2HD17NAEWeUXwmQh44uy32U+uutL+69e+6jjedfsddvSxx3m8xNNFQ67wipqQKHyESZ35
血清冻干粉 标准品 143 IU / ampoule 阿朴脂蛋白A-1 冻干粉 标准品 1.66mg / vial 阿朴脂蛋白B冻结品 标准品 1.22g / l. Vials. 1 ml. 精氨酸抗利尿激素冻干粉 标准品 8.2 IU / ampoule. 人心房利钠尿因子冻干粉 标准品 2.5 IU / ampoule. 第三页 枯草杆菌抗生素冻干粉 标准品 Approximately 100mg of zinc bacitracin (74IU/ mg) 碱性成纤维细胞生长因子 (bFGF
品 1.66mg / vial 阿朴脂蛋白B冻结品 标准品 1.22g / l. Vials. 1 ml. 精氨酸抗利尿激素冻干粉 标准品 8.2 IU / ampoule. 人心房利钠尿因子冻干粉 标准品 2.5 IU / ampoule. 第三页 枯草杆菌抗生素冻干粉 标准品 Approximately 100mg of zinc bacitracin (74IU/ mg) 碱性成纤维细胞生长因子 (bFGF, FGF-2)冻干粉 1,600 IU/ampoule. 卡介苗冻干粉 标准
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