| 名称 | Lacidipine |
| 描述 | Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure. |
| 体外活性 | Lacidipine, an L-type Ca(2+) channel blocker that also inhibits [Ca(2+)](ER) efflux, enhances folding, trafficking, and activity of degradation-prone glucocerebrosidase (GC) variants. Lacidipine remodels mutated GC proteostasis by simultaneously activating a series of distinct molecular mechanisms, namely modulation of Ca(2+) homeostasis, upregulation of the ER chaperone BiP, and moderate induction of the unfolded protein response. [1] Lacidipine almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages. [2] |
| 体内活性 | Lacidipine has non-significant effects on blood pressure but inhibits the paradoxical increases in plasma renin activity (PRA) and in renin mRNA in kidney that are found in salt-loaded stroke-prone spontaneously hypertensive rats (SHRSP). Lacidipine restores the physiological downregulation of renin production by high salt and reduces left ventricular hypertrophy and mRNA levels of atrial natriuretic factor and transforming growth factor-beta1. [3] Lacidipine (1 and 3 mg/kg) also effectively increases calcium concentrations significantly in ovariectomized rats. [4] Lacidipine, a dihydropyridine-type calcium antagonist, reduces the cardiac hypertrophy and the cardiacendothelin-1 (ET-1) gene overexpression occurring in salt-loaded stroke-prone spontaneously hypertensive rats (SL-SHRSP), an effect occurring without systolic blood pressure (SBP) change. Lacidipine exerts a dose-related inhibition of ventricle hypertrophy and preproET-1-mRNA expression in SHRSP and indicate that this effect is unrelated to SBP changes. [5] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 84 mg/mL (184.4 mM)
Ethanol : 21 mg/mL (46.1 mM)
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| 关键字 | Calcium Channel | inhibit | Ca2+ channels | hypertension | SN 305 | GX 1048 | Inhibitor | Lacidipine | SN305 | Reactive Oxygen Species | HKC cells | Ca channels | AKI | Caspase | Apoptosis | atherosclerosis | GX1048 |
| 相关产品 | Stavudine | Sodium 4-phenylbutyrate | Tributyrin |
| 相关库 | 疼痛相关化合物库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 抗癌临床化合物库 | 抗癌上市药物库 | 抗衰老化合物库 | 已知活性化合物库 | 离子通道库 | 抗癌药物库 |
United States
