Amiloride HCl

別名:MK-870 HCl

Amiloride HCl is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

Amiloride HCl化学構造

CAS No. 2016-88-8

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 23500 国内在庫あり
JPY 18100 国内在庫あり
JPY 101400 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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製品安全説明書

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Amiloride HCl関連製品

Sodium Channel阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 Amiloride HCl is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
Targets
Sodium channel [1] T-type calcium channel [2] uPA [3]
7 μM(Ki)
In Vitro
In vitro

Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 as low as 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC). [1]

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-AKT / AKT / p-PP1 / PP1 21694768
Immunofluorescence p53 30556178
In Vivo
In Vivo

Amiloride at 1 mg/kg/day subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP). compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension. [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

化学情報

分子量 266.09 化学式

C6H8ClN7O.HCl

CAS No. 2016-88-8 SDF --
Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl
保管

In vitro
Batch:

DMSO : 53 mg/mL ( (199.18 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 6 mg/mL

Ethanol : 5 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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