Amiloride HCl

製品コードS1811 バッチS181102

印刷

化学情報

Chemical Structure Synonyms MK-870 HCl Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C6H8ClN7O.HCl
分子量 266.09 CAS No. 2016-88-8
Solubility (25°C)* 体外 DMSO 53 mg/mL (199.18 mM)
Water 11 mg/mL (41.33 mM)
Ethanol 3 mg/mL (11.27 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 Amiloride HCl is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
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). [1]
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. [1]

プロトコル(参考用のみ)

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Amiloride alleviates morphine tolerance by suppressing ASIC3-dependent neuroinflammation in the spinal cord [ Eur J Pharmacol, 2023, 10.1016/j.ejphar.2023.176173] PubMed: 37918499
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Bile acids promote the caveolae-associated entry of swine acute diarrhea syndrome coronavirus in porcine intestinal enteroids [ PLoS Pathog, 2022, 18(6):e1010620] PubMed: 35696443
The sodium/glucose cotransporters as potential therapeutic targets for CF lung diseases revealed by human lung organoid swelling assay [ Mol Ther Methods Clin Dev, 2022, 24:11-19] PubMed: 34977268
Wireless Localized Electrical Stimulation Generated by an Ultrasound-Driven Piezoelectric Discharge Regulates Proinflammatory Macrophage Polarization [ Adv Sci (Weinh), 2021, 8(13):2100962] PubMed: 34258169

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。