计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
Lacidipine 是一种L-型钙离子通道抑制剂。A calcium channel protein inhibitor and blocker.
Information
Lacidipine Lacidipine (GX-1048, GR-43659X, SN-305) is a L-type calcium channel blocker, used for treating high blood pressure.
In vitro
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. Lacidipine almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages.
In vivo
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. Lacidipine (1 and 3 mg/kg) also effectively increases calcium concentrations significantly in ovariectomized rats. 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.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Lacidipine
生化机理
拉西地平（GX-1048、GR-43659X、SN-305）是一种 L 型钙通道阻滞剂，用于治疗高血压。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
638-759-0
分子类型
小分子
Isomeric SMILES
CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2/C=C/C(=O)OC(C)(C)C)C(=O)OCC)C)C
分子量
455.54
Reaxy-Rn
7395367
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7395367&ln=
高级数据
关联靶点（人）
CYP3A4
Tclin
细胞色素P450 3A4(Cytochrome P450 3A4)
(1 活性数据)
化学和物理性质
熔点
179 °C
安全和危险性（GHS）
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 B2310223 |
分析证书 | L409116 |
技术文档和文章
此产品的引用文献
溶液计算器
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