Amiloride HCl
别名: MK-870 HCl 中文名称：盐酸氨洛林
Amiloride HCl是一种选择性的T-type calcium channel阻滞剂，epithelial sodium channel（ENaC）阻滞剂，urokinase plasminogen activator (uPA)抑制剂，Ki=7 μM。
Amiloride HCl Chemical Structure
CAS: 2016-88-8
产品质控
批次：
纯度：
99.96%
99.96
Amiloride HCl相关产品
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| 相关化合物库 | FDA药物库 天然产物库 离子通道配体库 外泌体分泌相关化合物库 钙通道阻滞剂库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| YD-10B | Function assay | 4 mM | 4 h | amiloride strongly blocked the meridianin C‐induced accumulation of vacuoles in YD-10B cells | 30246484 |
| Dharma | Cell viability assay | 72 h | IC50=148.37 μM | 30556178 | |
| Abrams | Cell viability assay | 72 h | IC50=121.61 μM | 30556178 | |
| D17 | Cell viability assay | 72 h | IC50=110.66 μM | 30556178 | |
| NS20Y | Function assay | Amiloride dose dependently inhibits the ASIC current in NS20Y cells with an IC50 of 11.04 μM | 27342076 | ||
| COS-7 | Function assay | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells, Ki=3.28μM | 9258366 | ||
| COS-7 | Function assay | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells, Ki=11.6μM | 9258366 | ||
| COS-7 | Function assay | Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells, Ki=12μM | 9258366 | ||
| MDCK | Function assay | TP_TRANSPORTER: inhibition of TEA uptake in OCT2-expressing MDCK cells, Ki=4.7μM | 11758759 | ||
| MDCK | Function assay | TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing MDCK cells, Ki=6.9μM | 11758759 | ||
| AP1 | Function assay | Inhibition of Amphiuma tridactylum NHE1 mutant containing TM10-12 domain of Pleuronectes americanus expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol, IC50=38μM | 17493937 | ||
| AP1 | Function assay | Inhibition of Pleuronectes americanus NHE1 C-terminal mutant containing TM7 domain of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol | 17493937 | ||
| AP1 | Function assay | Inhibition of Pleuronectes americanus NHE1 TM4 mutant containing TFFLF sequence of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol | 17493937 | ||
| HBE | Function assay | Inhibition of human ENaC in HBE cells by short-circuit current technique, IC50=0.22μM | 22197144 | ||
| FRT | Function assay | Inhibition of guinea pig ENaCbeta1/gamma1 expressed in FRT cells by short-circuit current technique, IC50=0.54μM | 22197144 | ||
| HBE | Function assay | Blockade of human ENaC expressed in HBE cells by short-circuit current assay, IC50=0.22μM | 22425452 | ||
| FRT | Function assay | Blockade of guinea pig ENaC expressed in FRT cells by short-circuit current assay, IC50=0.54μM | 22425452 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| AP1 | Function assay | Inhibition of rat NHE1 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22Na+ influx by liquid scintillation spectroscopy, Ki=1μM | ChEMBL | ||
| AP1 | Function assay | Inhibition of full length human C-terminal HA-tagged human NHE5 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22NA+ influx by liquid scintillation spectroscopy, Ki=21μM | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Amiloride HCl是一种选择性的T-type calcium channel阻滞剂，epithelial sodium channel（ENaC）阻滞剂，urokinase plasminogen activator (uPA)抑制剂，Ki=7 μM。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Amiloride是上皮钠通道（ENaC的）的相对选择性抑制剂，IC 50为0.1 μM到0.5 μM。Amiloride是相对较差的Na+ / H +交换器（NHE）抑制剂，在外部钠离子浓度低时IC50低至3 μM，在外部钠离子浓度高时IC50高至1 mM。Amiloride是Na +/ Ca 2+交换（NCX）的弱抑制剂，IC 50为1 mM。Amiloride（1 μM）和Benzamil（30 nM）抑制血管收缩，通过阻断ENaC的蛋白质的活性抑制生肌响应于增加的灌注压力。在血管平滑肌细胞（VSMC）中，Amiloride完全抑制钠离子内流。[1] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AKT / AKT / p-PP1 / PP1 |
|
21694768 | |
| Immunofluorescence | p53 |
|
30556178 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在DOCA盐高血压大鼠中，Amiloride（1 mg/ kg /天，皮下注射）扭转初始胶原沉积的增加，并防止进一步增加。在盐水饮用，中风倾向的自发性高血压大鼠（SHRSP）中，Amiloride延迟蛋白尿的发作并改善脑和肾组织学分数。与对照组相比。在高血压盐依赖性动物中，Amiloride拮抗或阻止醛固酮在这些细胞以及血管和肾脏组织中的作用。[1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05044611 | Recruiting | Bipolar Disorder |
Assistance Publique - Hôpitaux de Paris |
January 11 2023 | Phase 4 |
| NCT04181008 | Completed | Pharmacokinetics |
University of Utah|Center for Addiction and Mental Health |
September 28 2020 | Early Phase 1 |
| NCT02323100 | Terminated | Cystic Fibrosis |
National Jewish Health|University of Alabama at Birmingham|Children''s Hospital of Philadelphia|Johns Hopkins University|Horizon Pharma Ireland Ltd. Dublin Ireland |
December 2 2018 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 266.09 | 分子式 | C6H8ClN7O.HCl |
| CAS号 | 2016-88-8 | SDF | -- |
| Smiles | C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 53 mg/mL ( (199.18 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 6 mg/mL (22.54 mM) Ethanol : 5 mg/mL (18.79 mM) |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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