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Amiloride hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Amiloride hydrochloride图片
CAS NO:2016-88-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
盐酸阿米洛利
MK-870 hydrochloride
产品介绍
Amiloride hydrochloride (MK-870 hydrochloride) 是上皮钠通道 (ENaC) 和尿激酶型纤溶酶原激活物受体 (uTPA) 的抑制剂。Amiloride hydrochloride 是polycystin-2(PC2;TRPP2) 通道阻断剂。
生物活性

Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelialsodium channel(ENaC[1]) and urokinase-type plasminogen activator receptor (uTPA[2]). Amiloride hydrochloride is a blocker ofpolycystin-2(PC2;TRPP2[3]) channel.

IC50& Target

ENaC[1]; uTPA[2]; polycystin-2(TRPP2)[3]

体外研究
(In Vitro)

Amiloride blocks δβγ channels with an IC50of 2.6 μM. The Kiof amiloride for δβγ ENaC is 26-fold that of αβγ channels (0.1 μM for αβγ ENaC). Amiloride blockade of δβγ ENaC is much more voltage dependent compared with the αβγ channel. The Kiof amiloride for δαβγ channels is 920 and 13.7 μM at –120 and+80 mV, respectively, which significantly differs from that of both αβγ and δβγ channels[1]. 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 IC50as 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 IC50of 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)[2].

体内研究
(In Vivo)

Amiloride (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[2].

Clinical Trial
分子量

266.09

性状

Solid

Formula

C6H9Cl2N7O

CAS 号

2016-88-8

中文名称

盐酸阿米洛利

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL(375.81 mM)

H2O : 7.14 mg/mL(26.83 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.7581 mL18.7906 mL37.5813 mL
5 mM0.7516 mL3.7581 mL7.5163 mL
10 mM0.3758 mL1.8791 mL3.7581 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (9.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (9.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.40 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (9.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.40 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。