拉西地平

Calcium Channel Inhibitors
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
L409116-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 GX-1048, GR-43659X, SN-305 | 4-​[2-​[(1E)​-​3-​(1,​1-​dimethylethoxy)​-​3-​oxo-​1-​propen-​1-​yl]​phenyl]​-​1,​4-​dihydro-​2,​6-​dimethyl-3,​5-​pyridinedicarboxylic acid 3,​5-​diethyl ester
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。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍

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%

关联靶点(人)

CYP3A4 Tclin 细胞色素P450 3A4(Cytochrome P450 3A4) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CCOC(=O)C1=C(C)NC(=C(C1C2=C(C=CC=C2)\C=C\C(=O)OC(C)(C)C)C(=O)OCC)C
分子量 455.54

安全和危险性(GHS)

技术规格说明书

concentration 9.0-11.0(mmol/L)
NMR Spectrum 1H Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo.  (2024)  Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection.  JOURNAL OF FOOD COMPOSITION AND ANALYSIS,  126  (17): (105825).  [PMID:17580304] [10.1016/j.jfca.2023.105825]
2. Y. Huang, P. Sun, Z. Zhang, C. Jin.  (2017)  Numerical method based on transfer function for eliminating water vapor noise from terahertz spectra.  APPLIED OPTICS,  56  (20): (5698-5704).  [PMID:29047713] [10.1364/AO.56.005698]

参考文献

1. Qinglin Wang, Hao Yuan, Xinyue Pan, Yiling Yang, Xiaosong Ma, Yahui Guo.  (2024)  Synthesis of silver nanoclusters using a double-stranded DNA template and its application for captopril detection.  JOURNAL OF FOOD COMPOSITION AND ANALYSIS,  126  (17): (105825).  [PMID:17580304] [10.1016/j.jfca.2023.105825]
2. Y. Huang, P. Sun, Z. Zhang, C. Jin.  (2017)  Numerical method based on transfer function for eliminating water vapor noise from terahertz spectra.  APPLIED OPTICS,  56  (20): (5698-5704).  [PMID:29047713] [10.1364/AO.56.005698]

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