Amiloride hydrochloride|2016-88-8|(盐酸阿米洛利; MK-870 hydrochloride)-陌孚医药/Medlife

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Amiloride hydrochloride (Synonyms: 盐酸阿米洛利; MK-870 hydrochloride)

目录号: PL11403 纯度: ≥99%

CAS No. :2016-88-8

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中文名称	Amiloride hydrochloride
中文别名	盐酸阿米洛利;阿米洛利;盐酸氨氯吡咪;氨氯吡咪;阿米洛利盐酸盐水合物;盐酸阿米洛利 EP标准品;盐酸阿米洛利标准品;盐酸阿米洛利二水;盐酸阿米洛利杂质;N-脒基-3,5-二氨基-6-氯吡嗪甲酰胺盐酸盐
英文名称	Amiloride hydrochloride
英文别名	amiloride hydrochloride hydrate;Amiloride Hydrochloride;Amiloride HCl;Amiloride (hydrochloride);Amiloride HCl dihydrate;AMILORIDE HYDROCHLORIDE, USP;MK-870 hydrochloride;3,5-diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide hydrochloride;3,5-Diamino-N-carbamimidoyl-6-chloropyrazine-2-carboxamide Hydrochloride Hydrate;AMILORIDE;amiloridechloride;Amiloridhydrochlorid;AMIPRAMIDIN;AMipraMidine;AMipraMizi;AMIPRAMIZIDE;amiprazidine;Arumil;GUANAMPRAZINE;HCL AMILORIDE HCL;N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride hydrate;N-Amido-3,5-diamino-6-chloropyrazine carboxamidehydrochloride;N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide hydrochloride;Amiloride chloride;Amiloride hydrochloride anhydrous;Amiloride, Hydrochloride;MLS000028442;Midamor;SMR000058414;N-Amidino-3,5-diamino-6-chloropyrazinecarboxamide monohydrochloride;DSSTox_CID_4452;DSSTox_RID_77402;Amiloride hydrochloride
Cas No.	2016-88-8
分子式	C₆H₉Cl₂N₇O
分子量	266.09
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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 epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

性状

Solid

IC50 & Target[1][2]

ENaC; uTPA; polycystin-2(TRPP2)

体外研究(In Vitro)

Amiloride blocks δβγ channels with an IC50 of 2.6 μM. 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 inhibi

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Ji, H.L., et al. delta ENaC: a novel divergent amiloride-inhibitable sodium channel. Am J Physiol Lung Cell Mol Physiol, 2012. 303(12): p. L1013-26.
[2]. Teiwes J, et al. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (375.81 mM)H₂O : 7.14 mg/mL (26.83 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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