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。