Amikacin disulfate.|39831-55-5|(阿米卡星硫酸盐; BAY 41-6551 disulfate)-陌孚医药/Medlife

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Amikacin disulfate. (Synonyms: 阿米卡星硫酸盐; BAY 41-6551 disulfate)

目录号: PC11670 纯度: ≥98%

CAS No. :39831-55-5

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中文名称	Amikacin disulfate.
中文别名	硫酸阿米卡星;硫酸丁胺卡那霉素;O-3-氨基-3-脱氧-alpha-D-葡吡喃糖基-(1→6)-O-[(6-氨基-6-脱氧-alpha-D-葡吡喃糖基-(1→4)]-N-(4-氨基-2-羟基-1-氧丁基)-2-脱氧-D-链霉胺硫酸盐;Amikacin sulfate salt 硫酸阿米卡星;阿米卡星;阿米卡星系统适用性 EP标准品;氨基羟丁基卡那霉素;丁胺卡那霉素二硫酸盐标准品;硫酸阿米卡星 EP标准品;硫酸阿米卡星 USP标准品;硫酸阿米卡星标准品;硫酸阿米卡星(硫酸丁胺卡那霉素);硫酸阿米卡星粉;硫酸丁胺卡那霉素阿米卡星;硫酸丁胺卡那霉素标准品;O-3-氨基-3-脱氧-alpha-D-葡吡喃糖基-(1→6)-O-[(6-氨基-6-脱氧-alpha-D-葡吡喃糖基-(1→4)]-N-(4-氨基-2-羟基-1-氧丁基)-2-脱氧-D-...;阿米卡霉素;阿米卡星杂质
英文名称	Amikacin disulfate
英文别名	Amikacin Sulphate;amikacin disulfate salt;4-amino-n-[5-amino-2-[4-amino-3,5-dihydroxy-6-(hydroxymethyl)tetrahydropyran-2-yl]oxy-4-[6-(aminomethyl)-3,4,5-trihydroxy-tetrahydropyran-2-yl]oxy-3-hydroxy-cyclohexyl]-2-hydroxy-butanamide disulfate salt;Amikacin sulfate salt;Amikacin disulfate;Amikacin Sulfate;BAY-416651 sulfate;(2S)-4-amino-N-{(1R,2S,3S,4R,5S)-5-amino-2-[(3-amino-3-deoxy-alpha-D-glucopyranosyl)oxy]-4-[(6-amino-6-;8-chloro-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione - 2-(diphenylmethoxy)-N,N-dimethylethanamine (1:1);Amikacin disulphate salt;Amikin sulfate;4-Amino-N-[5-amino-2-[4-amino-3,5-dihydroxy-6-(hydroxymethyl)tetrahydropyran-2-yl]oxy-4-[6-(aminomethyl)-3,4,5-trihydroxy-tetrahydropyran-2-yl]oxy-3-hydroxy-cyclohexyl]-2-hydroxy-butanamide disulfate;4-amino-N-[(2S,4S,5R)-5-amino-2-[(2S)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2S)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamidesulfuric acid;CID 134129615
Cas No.	39831-55-5
分子式	C₂₂H₄₇N₅O₂₁S₂
分子量	781.76
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Amikacin disulfate (BAY 41-6551 dissulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin disulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin disulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin disulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.

性状

Solid

IC50 & Target[1][2]

Aminoglycoside

体外研究(In Vitro)

Amikacin offers definite advantages for treating infections caused by organisms resistant to other aminoglycosides. Amikaci is affected by relatively few arninoglycoside-modifying enzymes. Amikacin is useful in the treatment of infections caused by Nocardia asteroides, Mycobacterium avium-intracellulare, and certain species of "rapid-growing" mycobacteria (that is, M. chelonae and M. fortuitumi).
Amikacin (100-1500 μM) causes a reliable dose-dependent loss of lateral line zebrafish hair cells with a LD₅₀ value of 453 μM.

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

体内研究(In Vivo)

Amikacin (320?mg/kg; subcutaneous injection; daily; for 10 days; male Fischer rats) treatment increases the chance of serious hearing loss in rats in vivo.

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

Animal Model:	Male Fischer 344 rats (40-50-day-old)
Dosage:	320?mg/kg
Administration:	Subcutaneous injection; daily; for 10 days
Result:	Induced hearing loss in rats.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

参考文献

[1]. Edson, R.S. and C.L. Terrell, The aminoglycosides. Mayo Clin Proc, 1999. 74(5): p. 519-28. [Information]

[2]. Ristuccia AM, et al. An overview of amikacin. Ther Drug Monit. 1985;7(1):12-25. [Information]

[3]. Sian R Kitcher, et al. ORC-13661 Protects Sensory Hair Cells From Aminoglycoside and Cisplatin Ototoxicity. JCI Insight. 2019 Aug 8;4(15):e126764. [Information]

溶解度数据

体外研究:

H₂O : 100 mg/mL (127.92 mM; Need ultrasonic)

DMSO : 1 mg/mL (1.28 mM; ultrasonic and warming and heat to 80°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2792 mL	6.3958 mL	12.7916 mL
5 mM	0.2558 mL	1.2792 mL	2.5583 mL
10 mM	0.1279 mL	0.6396 mL	1.2792 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (63.96 mM); Clear solution; Need ultrasonic

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产品使用指南

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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