Home Transmembrane Transporters Sodium Channel 억제제 Amiloride HCl

연구용

Amiloride HCl Sodium Channel 억제제

제품 번호: S1811

Amiloride HCl은 선택적인 T-type calcium channel 차단제이자 epithelial sodium channel 차단제이며, urokinase plasminogen activator (uPA)의 선택적 억제제(Ki=7 μM)입니다.
Amiloride HCl Sodium Channel 억제제 Chemical Structure

화학 구조

분자량: 266.09

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품질 관리 (Quality Control)

배치: 순도: 99.96%
99.96

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
D17 Cell viability assay 72 h IC50=110.66 μM 30556178
Abrams Cell viability assay 72 h IC50=121.61 μM 30556178
Dharma Cell viability assay 72 h IC50=148.37 μM 30556178
YD-10B Function assay 4 mM 4 h amiloride strongly blocked the meridianin C‐induced accumulation of vacuoles in YD-10B cells 30246484
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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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 266.09 화학식

C6H8ClN7O.HCl

 보관 (수령일로부터)
CAS 번호 2016-88-8 -- 원액 보관

동의어 MK-870 HCl Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 53 mg/mL (199.18 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 6 mg/mL

Ethanol : 5 mg/mL

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
Sodium channel
T-type calcium channel
uPA
7 μM(Ki)
시험관 내(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).

생체 내(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.

참조

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot p-AKT / AKT / p-PP1 / PP1
S1811-WB1
21694768
Immunofluorescence p53
S1811-IF1
30556178

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
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