Amiloride (MK-870) - CAS:2609-46-3

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Amiloride (MK-870) (Synonyms:3,5-二氨基-N-(氨基亚胺甲基)-6-氯-2-吡嗪甲酰胺;苯基硫代乙内酰脲-异亮氨酸(含苯基硫代乙内酰脲-别异亮氨酸);脒氯嗪;胍酰吡嗪)

目录号 : KG12666 CAS No. : 2609-46-3 纯度 : 98%

Data Sheet 产品使用指南

Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC), used in the management of hypertension and congestive heart failure. Amiloride blocks δβγ channels with an IC50 of 2.6 μM (58, 71, 75, 134, 148). The Ki of 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 Ki of 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. 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). 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.

规格	价格	是否有货	数量
100mg		In-stock	立即试用

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分子式

C₆H₈ClN₇O

分子量

229.63

CAS号

2609-46-3

中文名称

胍酰吡嗪

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (435.48 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.3548 mL	21.7741 mL	43.5481 mL
5 mM	0.8710 mL	4.3548 mL	8.7096 mL
10 mM	0.4355 mL	2.1774 mL	4.3548 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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 (10.89 mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (10.89 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 μ L Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。
2.

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

Solubility:≥ 2.5 mg/mL (10.89 mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (10.89 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 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility:≥ 2.5 mg/mL (10.89 mM); Clear solution

此⽅案可获得 ≥ 2.5 mg/mL (10.89 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。