盐酸地尔硫卓 ≥98%
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| 熔点: | 212-214 oC |
| 外观与性状: | 白色或类白色的结晶或结晶性粉末 |
| 包装规格: | 1g 5g 25g in poly bottle |
| 产品简介: | 一种Diltiazem hydrochloride是钙离子流入抑制剂(缓慢通道阻断剂或钙拮抗剂)。 |
| 溶解性: | 溶于水、甲醇和三氯甲烷。 |
| 储备液保存: | -80°C, 6 months -20°C, 1 month (sealed storage, away from moisture) |
| 体内实验: | 1、请依序添加每种溶剂: PBS Solubility: 100 mg/mL (221.73 mM); 澄清溶液; 超声助溶 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
| 靶点: | L-type calcium channel |
| 体外研究: | Benzothiazepine Ca2+ antagonist diltiazem hydrochloride interacts with transmembrane segments IIIS6 and IVS6 in the α1 subunit of L-type Ca2+ channels. Diltiazem causes a dose-dependent inhibiton of contractions as well as Ca2+ influx stimulated by alpha adrenoceptor activation and high-K+ depolarization. Diltiazem is roughly equally potent in inhibiting contractions induced by high-K+ and a low concentration of norepinephrine (NE). Diltiazem also inhibits the Na-dependent Ca-efflux from heart mitochondria. Both the (+)-optical isomers of the cis- and trans-forms of diltiazem inhibit Na-Ca exchange activity with comparable potency (IC50 of 10-20 μM). |
| 体内研究: | Diltiazem produces a noncompetitive inhibition of Ca2+-induced contractions of depolarized rabbit aorta. Furthermore, there is a lack of parallelism between the smooth muscle effects of removal of [Ca2+]ex and of addition of diltiazem. Diltiazem improves the cardiac microcirculation and function in an experimental model of hyperthyroidism in rats. The treatment of hyperthyroid rats with losartan diltiazem (4.7±0.7%; P < 0.001) significantly reduces the percentage of fibrosis areas in the left ventricle . In conscious spontaneously hypertensive rats (SHR), diltiazem dose-dependently decreases the blood pressure and increases the heart rate after intravenous administration (0.03--1 mg/kg). Oral administration of diltiazem (100 mg/kg) also reduces the blood pressure of SHR. |
| 保存条件: | 2-8℃ |
| 注意事项: | 1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。 |
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