硫酸阿米卡星 | 39831-55-5

• 物质功能分类: 原料药 - 抗生素类药物 - 其它抗生素类药
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 硫酸阿米卡星
• 中文别名: 硫酸丁胺卡那霉素；地佐环平；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)]-
• 英文名称: amikacin Sulfate
• 英文别名: amikacin sulphate；(2S)-4-amino-N-[(1R,2S,3S,4R,5S)-5-amino-2-[(2S,3R,4S,5S,6R)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2R,3R,4S,5S,6R)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamide;sulfuric acid
• CAS: 39831-55-5
• 化学式: C₂₂H₄₃N₅O₁₃*H₂O₄S
• 分子量: 683.689
• InChiKey: HIBICIOPDUTNRR-XTHCGPPUSA-N

物化性质

• 熔点：
  220-230 C
• 比旋光度：
  D22 +74.75° (water)
• 溶解度：
  H2O：50 mg/mL，澄清，无色
• 稳定性/保质期：
  常规情况下不会分解，也没有危险反应。

计算性质

• 辛醇/水分配系数(LogP)：
  -9.08
• 重原子数：
  45
• 可旋转键数：
  10
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.95
• 拓扑面积：
  415
• 氢给体数：
  15
• 氢受体数：
  21

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S26,S36
• 危险类别码：
  R36/37/38
• WGK Germany：
  2
• 海关编码：
  29419000
• 危险品运输编号：
  NONH for all modes of transport
• RTECS号：
  WK1961200
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335,H351,H361
• 储存条件：
  密封、阴凉、干燥保存。

SDS

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Section 1. Chemical Product and Company Identification
Amikacin sulfate Catalog
A1309, A1624, YY223
Common Name/
Number(s).
Trade Name
CAS# 39831-55-5
Manufacturer
RTECS WK1961200
SPECTRUM QUALITY PRODUCTS INC.
TSCA TSCA 8(b) inventory: No
products were found.
Commercial Name(s) Not available.
CI# Not available.
Synonym O-3-Amino-3-deoxy-alpha-D-glucopyranosyl-(1-6)-O-(6-amino-6-deoxy-alpha-D-glucopyranosyl-(1-4))-N(sup
1)-(4-amino-2-hydroxy-1-oxobutyl)-2-deoxy-(S)-D-streptamine sulfate IN CASE OF EMERGENCY
(1:2) salt
Chemical Name Not available.
Not available. CALL [phone]
Chemical Family
Chemical Formula C22H43N5O13.2H2SO4
SPECTRUM QUALITY PRODUCTS INC.

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Section 2.Composition and Information on Ingredients
Exposure Limits
TWA (mg/m3) STEL (mg/m3) CEIL (mg/m3)
Name CAS # % by Weight
1) Amikacin sulfate 39831-55-5 100
Toxicological Data Amikacin sulfate:
on Ingredients ORAL (LD50): Acute: 4001 mg/kg [Rat]. 10679 mg/kg [Mouse]. 3001 mg/kg [Rabbit].

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Section 3. Hazards Identification
Potential Acute Health Effects Hazardous in case of skin contact (irritant), of eye contact (irritant), of ingestion. Slightly hazardous in case of
inhalation.
Potential Chronic Health CARCINOGENIC EFFECTS: Not available.
MUTAGENIC EFFECTS: Not available.
Effects
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Not available.
Repeated or prolonged exposure is not known to aggravate medical condition.
Amikacin sulfate

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Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for at
least 15 minutes. Cold water may be used. Get medical attention.
Skin Contact In case of contact, immediately flush skin with plenty of water. Cover the irritated skin with an emollient. Remove
contaminated clothing and shoes. Cold water may be used.Wash clothing before reuse. Thoroughly clean shoes
before reuse. Get medical attention.
Serious Skin Contact Wash with a disinfectant soap and cover the contaminated skin with an anti-bacterial cream. Seek medical
attention.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get
medical attention.
Serious Inhalation Not available.
Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an
unconscious person. Loosen tight clothing such as a collar, tie, belt or waistband. Get medical attention if
symptoms appear.
Serious Ingestion Not available.

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Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points Not available.
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), sulfur oxides (SO2, SO3...).
Fire Hazards in Presence of Not available.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
of Various Substances Risks of explosion of the product in presence of static discharge: Not available.
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on Not available.
Fire Hazards
Special Remarks on Explosion Not available.
Hazards

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Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. If necessary: Neutralize
the residue with a dilute solution of sodium carbonate. Finish cleaning by spreading water on the
contaminated surface and dispose of according to local and regional authority requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Neutralize the residue with a dilute
solution of sodium carbonate. Finish cleaning by spreading water on the contaminated surface and allow to
evacuate through the sanitary system.
Amikacin sulfate

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Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Empty containers pose a fire risk, evaporate the
residue under a fume hood. Ground all equipment containing material. Do not ingest. Do not breathe dust.
Wear suitable protective clothing. If ingested, seek medical advice immediately and show the container or the
label. Avoid contact with skin and eyes.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area.

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Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection Splash goggles. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent.
Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used
a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist
BEFORE handling this product.
Exposure Limits Not available.

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Section 9. Physical and Chemical Properties
Physical state and appearance Solid. Odor Not available.
Not available.
Taste
Molecular Weight 781.77 g/mole
Not available.
Color
3 [Acidic.]
pH (1% soln/water)
Boiling Point Not available.
Melting Point Decomposition temperature: 220°C (428°F)
Critical Temperature Not available.
Specific Gravity Not available.
Not applicable.
Vapor Pressure
Vapor Density Not available.
Not available.
Volatility
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties See solubility in water.
Solubility Partially soluble in cold water.

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Section 10. Stability and Reactivity Data
Stability The product is stable.
Instability Temperature Not available.
Conditions of Instability Not available.
Incompatibility with various Not available.
substances
Corrosivity Not available.
Amikacin sulfate
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization Will not occur.

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Section 11. Toxicological Information
Routes of Entry Eye contact. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 3001 mg/kg [Rabbit].
Chronic Effects on Humans Not available.
Other Toxic Effects on Hazardous in case of skin contact (irritant), of ingestion.
Humans Slightly hazardous in case of inhalation.
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on Not available.
Chronic Effects on Humans
Special Remarks on other Not available.
Toxic Effects on Humans

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Section 12. Ecological Information
Not available.
Ecotoxicity
BOD5 and COD Not available.
Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation products may
arise.
Toxicity of the Products The products of degradation are more toxic.
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

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Section 13. Disposal Considerations
Waste Disposal

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Identification Not applicable.
Not applicable.
Special Provisions for
Transport
DOT (Pictograms)
Amikacin sulfate

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Section 15. Other Regulatory Information and Pictograms
California prop. 65: This product contains the following ingredients for which the State of California has found to
Federal and State
cause cancer, birth defects or other reproductive harm, which would require a warning under the statute:
Regulations
Amikacin sulfate
California prop. 65: This product contains the following ingredients for which the State of California has found to
cause birth defects which would require a warning under the statute: Amikacin sulfate
California
California prop. 65: This product contains the following ingredients for which the State of California has found
Proposition 65
to cause birth defects which would require a warning under the statute: Amikacin sulfate
Warnings
Other Regulations Not available.
WHMIS (Canada) Not controlled under WHMIS (Canada).
Other Classifications
DSCL (EEC) R36/38- Irritating to eyes and skin.
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.
Splash goggles.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

概述

硫酸丁胺卡那霉素是一种半合成氨基糖苷类抗生素，其抗菌谱与庆大霉素相似。它对金黄色葡萄球菌、绿脓杆菌、大肠杆菌及变形杆菌等均有疗效，并且对其他氨基糖甙类抗生素耐药的细菌也有治疗效果。

生物活性

Amikacin sulfate（BB-K8）是一种半合成、水溶性的卡那霉素氨基糖苷衍生物，能够结合到细菌30S核糖体亚基上，导致mRNA错误翻译，从而使细菌无法合成其生长所需的蛋白质。

靶点

Target	Value
16S rRNA

体外研究

Amikacin sulfate对细菌30S核糖体的16S rRNA具有高亲和力，导致mRNA错误翻译，并使细菌无法合成对其生长至关重要的蛋白质。体外研究表明，amikacin sulfate对假单胞菌属、大肠杆菌、变形杆菌（包括吲哚阳性和阴性）、普罗维登斯菌属、克雷伯菌-肠杆菌-沙雷氏菌属、不动杆菌属和弗氏柠檬酸杆菌具有活性。此外，体外研究还表明，amikacin sulfate与β-内酰胺抗生素协同作用于许多临床重要的革兰氏阴性细菌，包括与莫西沙星或哌拉西林联合使用时表现出更显著的效果。

体内研究

在实验性兔子心内膜炎模型中，阿米卡星（80 mg/kg i.v.）显著减少了主动脉瓣赘生物的假单胞菌密度。每天一次给药比每天两次给药更为有效。同时，在禽结核分枝杆菌复合物感染模型中，以50 mg/kg剂量单独或分次给药表现出显著活性，并且加入氯法齐明后活性进一步增强。

用途

硫酸阿米卡星是一种抗感染药物，用于治疗由敏感菌引起的尿路感染、败血症、皮肤感染、骨与关节感染、肺炎及下呼吸道感染等。

类别

有毒物品

毒性分级

中毒

急性毒性

• 口服 - 大鼠 LD50：＞4000 mg/kg
• 腹腔 - 小鼠 LD50：2930 mg/kg

可燃性危险特性

可燃；燃烧时产生有毒氮氧化物和硫氧化物烟雾

储运特性

库房应通风、低温干燥

灭火剂

干粉、泡沫、沙土、二氧化碳、雾状水

反应信息

• 作为反应物：
  描述：

  硫酸阿米卡星 在 OH— 、 resultant solution 作用下， 以 水 为溶剂， 反应 1.0h， 生成 阿米卡星
  参考文献：
  名称：

  ANTIBACTERIAL 4,6-SUBSTITUTED 6', 6'' AND 1 MODIFIED AMINOGLYCOSIDE ANALOGS

  摘要：

  本发明涉及氨基糖苷化合物的类似物，以及它们的制备和用作预防或治疗微生物感染的药物。

  公开号：

  US20130144044A1
• 作为产物：
  描述：

  阿米卡星 在 硫酸 作用下， 以 乙醇 、 水 为溶剂， 反应 6.0h， 以91.5%的产率得到硫酸阿米卡星
  参考文献：
  名称：

  一种硫酸阿米卡星化合物

  摘要：

  本发明公开了一种硫酸阿米卡星化合物，该化合物用粉末X射线衍射测定法测定，以2θ±0.2°衍射角表示在6.3°，13.0°，14.3°，17.2°，18.2°，20.0°，22.7°，23.7°，25.9°，27.5°，29.2°处显示出特征衍射峰。本发明制备的硫酸阿米卡星化合物具有稳定性好、纯度高、杂质少的优点，而且工艺简单，收率高，重复性强，用药安全性和有效性高，大大降低了不良反应的发生率，适合于工业化生产。

  公开号：

  CN110862424A

文献信息

• [EN] PEPTIDE-BASED MULTIPLE-DRUG DELIVERY VEHICLE<br/>[FR] VÉHICULE D'ADMINISTRATION DE MÉDICAMENTS MULTIPLES À BASE DE PEPTIDES
  申请人：ARIEL-UNIVERSITY RES AND DEV COMPANY LTD

  公开号：WO2017068577A1

  公开（公告）日：2017-04-27

  A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

  本文提供了一种包括靶向基团、多功能肽平台和附着在其上的多种可控释放的生物活性剂的分子结构。
• ANTHELMINTIC COMPOUNDS AND COMPOSITIONS AND METHOD OF USING THEREOF
  申请人：Meng Charles Q.

  公开号：US20140142114A1

  公开（公告）日：2014-05-22

  The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 and X 8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.

  本发明涉及以下式（I）的新型驱虫化合物： 其中 Y和Z分别是双环碳环或双环杂环基团，或者Y或Z中的一个是双环碳环或双环杂环基团，另一个是烷基，烯基，炔基，环烷基，苯基，杂环基或杂芳基，以及变量X 1 ，X 2 ，X 3 ，X 4 ，X 5 ，X 6 ，X 7 和X 8 如本文所定义。本发明还提供了包含本发明的驱虫化合物的兽药组合物，以及它们用于治疗和预防动物寄生虫感染的用途。
• [EN] ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS<br/>[FR] COMPOSÉS DEPSIPEPTIDIQUES ANTHELMINTHIQUES
  申请人：MERIAL INC

  公开号：WO2018093920A1

  公开（公告）日：2018-05-24

  The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy1, Cy2, R1, R2, R3, R4, Ra and Rb is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

  本发明提供了公式（I）的环状脱氨肽化合物，其中至少一个碳原子的立体化学构型与自然存在的环状脱氨肽PF1022A的基团Cy1、Cy2、R1、R2、R3、R4、Ra和Rb相比发生了倒置。该发明还提供了包含这些化合物的组合物，对危害动物的寄生虫具有有效性。这些化合物和组合物可用于对抗哺乳动物和鸟类体内或体表的寄生虫。该发明还提供了一种改进的方法，用于根除、控制和预防鸟类和哺乳动物的寄生虫感染。
• HIV protease inhibiting compounds
  申请人：Flentge Charles A.

  公开号：US20110003827A1

  公开（公告）日：2011-01-06

  A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

  公开了一种具有以下公式的化合物，作为HIV蛋白酶抑制剂。还公开了抑制HIV感染的方法和组合物。
• [EN] HIV PROTEASE INHIBITING COMPOUNDS<br/>[FR] COMPOSES INHIBITEURS DE LA PROTEASE DU VIH
  申请人：ABBOTT LAB

  公开号：WO2005061487A1

  公开（公告）日：2005-07-07

  A compound of the formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

  公开了一种公式(I)的化合物作为HIV蛋白酶抑制剂。还公开了用于抑制HIV感染的方法和组合物。