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Submit ReviewAmiloride hydrochloride
说明： Na+ channel blocker; also I2 imidazoline ligand
化学名： 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide hydrochloride
纯度： ≥98% (HPLC)
生物活性 for Amiloride hydrochloride
Amiloride hydrochloride is a Na+ channel blocker. Defines the I2A-amiloride sensitive and I2B-amiloride insensitive imidazoline binding Blocks TRPP3, acid sensing- (ASIC) and mechanogated membrane-ion channels, as well as the Na+/H+ exchanger. Also inhibits urokinase-type plasminogen activator (uPA); has no effect on tissue-type plasminogen activator.
技术数据 for Amiloride hydrochloride
| 分子量 | 266.09 |
| 公式 | C6H8ClN7O.HCl |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2016-88-8 |
| PubChem ID | 16230 |
| InChI Key | ACHKKGDWZVCSNH-UHFFFAOYSA-N |
| Smiles | Cl.NC(=N)NC(=O)C1=NC(Cl)=C(N)N=C1N |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Amiloride hydrochloride
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 1.33 | 5 温和加热 | |
| DMSO | 26.61 | 100 |
制备储备液 for Amiloride hydrochloride
以下数据基于产品分子量 266.09。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.76 mL | 18.79 mL | 37.58 mL |
| 5 mM | 0.75 mL | 3.76 mL | 7.52 mL |
| 10 mM | 0.38 mL | 1.88 mL | 3.76 mL |
| 50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
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产品说明书 for Amiloride hydrochloride
参考文献 for Amiloride hydrochloride
参考文献是支持产品生物活性的出版物。
Dai et al (2007) Inhibition of TRPP3 channel by amil. and analogs. Mol.Pharmacol. 72 1576 PMID: 17804601
Hamill and McBride (1996) The pharmacology of mechanogated membrane ion channels. Pharmacol.Rev. 48 231 PMID: 8804105
Kleyman et al (1988) Amiloride and its analogues as tools in the study of ion transport. J.Membr.Biol. 105 1 PMID: 2852254
Ernsberger et al (1992) A second generation of centrally acting antihypertensive agents act on putative I1-imidazoline receptors. J.Cardiovasc.Pharmacol. 20 S1
Jetti et al (2010) Evaluation of the role of nitric oxide in acid sensing ion channel mediated cell death. Nitric Oxide 22 213 PMID: 20045740
Vassalli et al (1987) Amiloride selectively inhibits the urokinase-type plasminogen activator. 214 187 PMID: 3106085
If you know of a relevant reference for Amiloride hydrochloride, please let us know.
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关键词: Amiloride hydrochloride, Amiloride hydrochloride supplier, I2, selective, ligands, differentiates, I2A, I2B, Na+, channel, blockers, Imidazoline, Receptors, Sodium, NaV, Channels, voltage-gated, voltage-dependent, NHE, H+, exchanger, ASIC, upa, urokinase-type, plasminogen, inhibitors, inhibits, Voltage-gated, Na+/H+, Exchanger, TRPP, Urokinase, 0890, Tocris Bioscience
7 篇 Amiloride hydrochloride 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Amiloride hydrochloride 的部分引用包括：
Neubert et al (2020) NCX1 Represents an Ionic Na+ Sensing Mechanism in Macrophages PloS Biol 18 PMID: 32569301
Roebber et al (2019) The Role of the Anion in Salt (NaCl) Detection by Mouse Taste Buds. J Neurosci 39 6224 PMID: 31171579
Messerschmidt et al (2019) Osmotic induction of cyclooxygenase-2 in RPE cells: Stimulation of inflammasome activation. Mol Vis 25 329 PMID: 31341381
Barbaro (2017) Dendritic cell amiloride-sensitive channels mediate sodium-induced inflammation and hypertension. Cell Rep 21 1009 PMID: 29069584
Korang-Yeboah et al (2015) Polycaprolactone/maltodextrin nanocarrier for intracellular drug delivery: formulation, uptake mechanism, internalization kinetics, and subcellular localization. J Neurosci 10 4763 PMID: 26251597
Poon et al (2018) Effects of the potassium-sparing diuretic amil. on chemotherapy response in canine osteosarcoma cells. J Vet Intern Med 33 800 PMID: 30556178
Jeong et al (2013) Antinociceptive effects of amil. and benzamil in neuropathic pain model rats. Int J Nanomedicine 28 1238 PMID: 23960454
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Amiloride hydrochloride 的评论
平均评分: 4 (基于 2 条评论。)
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Drug treatments.
By
Andrew Poon on 03/01/2019
分析类型： In Vitro
种属： Other
Amiloride was combined with chemotherapy to assess its potential to kill canine osteosarcoma cells, and was found to be synergistic with doxorubicin chemotherapy. It was also used by the Seahorse analyzer to show that the extracellular acidification rate (ECAR) decreases after amiloride exposure.
Dissolve the powder in 100 mM DMSO, and dilute according to minimize vehicle effects.
ASIC inhibition on acute brain slices.
By
Anonymous on 01/10/2018
分析类型： In Vivo
种属： Mouse
细胞系/组织： acute brain slice
Used to show ASIC channels were not involved in the studied effect. No effect was had, as expected, however it's hard to control for the drug efficacy as we did not show ASIC blockade directly.