阿折地平
货号：
IA3730
品牌：
Jinpan
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产品简介
| 描述 | 是二氢吡啶衍生物，为L型钙离子通道阻断剂。 |
| MDL | MFCD00865803 |
| EC | EINECS 634-143-0 |
| 别名 | RS-9054 |
| 英文名称 | Azelnidipine |
| CAS | 123524-52-7 |
| 分子式 | C33H34N4O6 |
| 分子量 | 582.65 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | Azelnidipine是一种二氢吡啶类钙通道阻断剂。[1] |
| In Vitro | Azelnidipine是一种新开发的长效钙通道阻断剂，具有独特的药理学特性，例如使心跳减慢和对维管组织的高亲和力，这些特性使它与其它的钙通道阻断剂有所不同，因此Azelnidipine成为新一代钙通道阻断剂可以用来治疗高血压，不管病人是否具有缺血性心脏病的风险。由于它的高脂溶性使得它从血液中被清除后仍然可以留在血管壁当中继续发挥降血压的功效。[1] |
| In Vivo | AZL itself exhibited little effect on myocyte mechanics but it significantly alleviated STZ-induced myocyte contractile dysfunction. All of these STZ-induced alterations were reconciled by AZL treatment. Collectively, the data suggest beneficial effect of AZL in diabetic cardiomyopathy via altering intracellular Ca2+ handling proteins and preventing apoptosis by its antioxidant property.[2] |
| SMILES | O=C(C1=C(N)NC(C)=C(C(OC(C)C)=O)C1C2=CC=CC([N+]([O-])=O)=C2)OC3CN(C(C4=CC=CC=C4)C5=CC=CC=C5)C3 |
| 靶点 | Calcium Channel |
| 细胞实验 | Six to eight-week-old male Wistar rats (NCCS, Pune,India), weighing 250 to 280 g, were made diabetic by single intra-peritoneal (IP) injection of streptozotocin (STZ) (55 mg/kg). Control animals were treated with vehicle (0.1 mol/L sodium citrate buffer, pH4.5). Hyperglycemia (blood glucose > 200 mg/dL) was confirmed 3 days post STZ injection using a glucometer. Diabetic animals were treated with single dose of 5 mg/kg AZL suspended in 1% carboxy methyl cellulose, administered orally by gavage, starting the 4th day of STZ treatment (n = 12) daily for a period of 12 weeks. Blood glucose and body weight were measured weekly and at the end of the study.[2] |
| 数据来源文献 | [1]. Komoda H, Inoue T, Node K. Anti-inflammatory properties of azelnidipine, a dihydropyridine-based calcium channel blocker. Clin Exp Hypertens. 2010 Jan;32(2):121-8. [2]. Kain V, Kumar S, Sitasawad SL. Azelnidipine prevents cardiac dysfunction in streptozotocin-diabetic rats by reducing intracellular calcium accumulation, oxidative stress and apoptosis. Cardiovasc Diabetol. 2011 Nov 4;10:97. |
| 规格 | 5mg 10mg 10mM*1mL in DMSO |