生物活性
Olmesartan medoxomil (Benicar) is a compound which is hydrolyzed to olmesartan that is a selective AT1 subtype angiotensin II receptor antagonist.Olmesartan medoxomil (Benicar) was converted to olmesartan? during absorption from the gastrointestinal tract. Olmesartan is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. Olmesartan medoxomil (Benicar) exerts its pharmacological functions via blocking the binding of angiotensin II to the AT1 receptors in vascular muscle; it is therefore independent of angiotensin II synthesis pathways, unlike ACE inhibitors. By blocking the binding rather than the synthesis of angiotensin II, olmesartan prevents the negative regulatory feedback on renin secretion. As a result of this blockage, olmesartan attenuates vasoconstriction and the secretion of aldosterone. Olmesartan lowers blood pressure by producing vasodilation, and decreasing peripheral resistance.
化学数据
| 分子量 | 558.59 |
| 分子式 | C29H30N6O6 |
| CAS号 | 144689-63-4 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 80 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7902 mL | 8.9511 mL | 17.9022 mL |
| 5 mM | 0.358 mL | 1.7902 mL | 3.5804 mL |
| 10 mM | 0.179 mL | 0.8951 mL | 1.7902 mL |
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