Amiloride HCl

別名: MK-870 HCl 中文名稱：鹽酸氨洛林

目錄號：S1811 Purity: 99.96%

Amiloride HCl是一種選擇性的T-type calcium channel阻滯劑，epithelial sodium channel（ENaC）阻滯劑，urokinase plasminogen activator (uPA)抑制劑，Ki=7 μM。

Amiloride HCl Chemical Structure

CAS: 2016-88-8

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1073.86	現(xiàn)貨
50mg	783.74	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產(chǎn)品質控

批次：純度： 99.96%

99.96

Amiloride HCl相關產(chǎn)品

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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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
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生物活性

產(chǎn)品描述

Amiloride HCl是一種選擇性的T-type calcium channel阻滯劑，epithelial sodium channel（ENaC）阻滯劑，urokinase plasminogen activator (uPA)抑制劑，Ki=7 μM。

靶點

Sodium channel ^[1]	T-type calcium channel ^[2]	uPA ^[3]
		7 μM(Ki)

體外研究(In Vitro)
體外研究活性	Amiloride是上皮鈉通道（ENaC的）的相對選擇性抑制劑，IC 50為0.1 μM到0.5 μM。Amiloride是相對較差的Na+ / H +交換器（NHE）抑制劑，在外部鈉離子濃度低時IC50低至3 μM，在外部鈉離子濃度高時IC50高至1 mM。Amiloride是Na +/ Ca 2+交換（NCX）的弱抑制劑，IC 50為1 mM。Amiloride（1 μM）和Benzamil（30 nM）抑制血管收縮，通過阻斷ENaC的蛋白質的活性抑制生肌響應于增加的灌注壓力。在血管平滑肌細胞（VSMC）中，Amiloride完全抑制鈉離子內流。^[1]
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	p-AKT / AKT / p-PP1 / PP1		21694768
	Immunofluorescence	p53		30556178

體內研究(In Vivo)
體內研究活性	在DOCA鹽高血壓大鼠中，Amiloride（1 mg/ kg /天，皮下注射）扭轉初始膠原沉積的增加，并防止進一步增加。在鹽水飲用，中風傾向的自發(fā)性高血壓大鼠（SHRSP）中，Amiloride延遲蛋白尿的發(fā)作并改善腦和腎組織學分數(shù)。與對照組相比。在高血壓鹽依賴性動物中，Amiloride拮抗或阻止醛固酮在這些細胞以及血管和腎臟組織中的作用。^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05044611	Recruiting	Bipolar Disorder	Assistance Publique - H?pitaux 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

參考文獻
[1] Teiwes J, et al. Am J Hypertens, 2007, 20(1), 109-117. [2] Tang CM, et al. Science. 1988, 240(4849):213-5. [3] Vassalli JD, et al. FEBS Lett. 1987, 214(1):187-91.

參考文獻

[1] Teiwes J, et al. Am J Hypertens, 2007, 20(1), 109-117.
[2] Tang CM, et al. Science. 1988, 240(4849):213-5.
[3] Vassalli JD, et al. FEBS Lett. 1987, 214(1):187-91.

化學信息&溶解度

分子量	266.09	分子式	C₆H₈ClN₇O.HCl
CAS號	2016-88-8	SDF	--
Smiles	C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.Cl
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 53 mg/mL ( (199.18 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 6 mg/mL (22.54 mM)

Ethanol : 5 mg/mL (18.79 mM)

DMSO : 53 mg/mL ( (199.18 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 11 mg/mL (41.33 mM)

Ethanol : 3 mg/mL (11.27 mM)

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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