fusidic acid sodium salt | 751-94-0

• 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 - 脂质和类脂质分子 - 类固醇和类固醇衍生物
• 英文名称: fusidic acid sodium salt
• 英文别名: sodium fusidate；fucidin；fusidate sodium；Fucidina；sodium;(2Z)-2-[(3R,4S,5S,8S,9S,10S,11R,13R,14S,16S)-16-acetyloxy-3,11-dihydroxy-4,8,10,14-tetramethyl-2,3,4,5,6,7,9,11,12,13,15,16-dodecahydro-1H-cyclopenta[a]phenanthren-17-ylidene]-6-methylhept-5-enoate
• CAS: 751-94-0
• 化学式: C₃₁H₄₇O₆*Na
• 分子量: 538.7
• InChiKey: HJHVQCXHVMGZNC-JCJNLNMISA-M

物化性质

• 熔点：
  >200°C (dec.)
• 溶解度：
  可溶于水中

计算性质

• 辛醇/水分配系数(LogP)：
  1.34
• 重原子数：
  38
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.81
• 拓扑面积：
  107
• 氢给体数：
  2
• 氢受体数：
  6

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S26,S36
• 危险类别码：
  R22
• WGK Germany：
  3
• 海关编码：
  2942000000
• RTECS号：
  LV5775000
• 储存条件：
  2-8°C条件下应密封储存。

SDS

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Section 1. Chemical Product and Company Identification
Fusidic Acid Sodium Salt
Common Name/
Trade Name
Manufacturer
Commercial Name(s)
Synonym
Chemical Name
Chemical Family
Fusidic Acid Sodium Salt

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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 if irritation occurs.
Skin Contact Wash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation
develops. Cold water may be used.
Serious Skin Contact Not available.
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. If large quantities of this material are swallowed, call a physician immediately.
Loosen tight clothing such as a collar, tie, belt or waistband.
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.
Not available.
Flash Points
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2). Some metallic oxides.
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances
Risks of explosion of the product in presence of mechanical impact: Not available.
Explosion Hazards in
Risks of explosion of the product in presence of static discharge: Not available.
Presence of Various
Substances
SMALL FIRE: Use DRY chemical powder.
Fire Fighting Media
LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
and Instructions
Special Remarks on Material in powder form, capable of creating a dust explosion. As with most organic solids, fire is possible at
elevated temperatures
Fire Hazards
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presence of an ignition source is a potential
dust explosion hazard.
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. 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. Finish cleaning by spreading
water on the contaminated surface and allow to evacuate through the sanitary system.

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Section 7. Handling and Storage
Keep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do
Precautions
not ingest. Do not breathe dust. Wear suitable protective clothing. If ingested, seek medical advice
immediately and show the container or the label. Keep away from incompatibles such as oxidizing agents.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area. Do not store above 8°C
(46.4°F). Refrigerate.
Fusidic Acid Sodium Salt

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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 Safety glasses. 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
a Large Spill used 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. (Powdered solid.) Odor Not available.
Taste Not available.
Molecular Weight 538.7g/mole
White. Off-white.
Color
Not available.
pH (1% soln/water)
Boiling Point Not available.
Not available.
Melting Point
Critical Temperature Not available.
Not available.
Specific Gravity
Vapor Pressure Not applicable.
Vapor Density Not available.
Not available.
Volatility
Odor Threshold Not available.
Not available.
Water/Oil Dist. Coeff.
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.
Not available.
Instability Temperature
Conditions of Instability Excess heat, incompatible materials, dust generation
Incompatibility with various Reactive with oxidizing agents.
substances
Corrosivity Not available.
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization Will not occur.
Fusidic Acid Sodium Salt

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Section 11. Toxicological Information
Routes of Entry Inhalation. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 840.5 mg/kg [Mouse].
Chronic Effects on Humans Not available.
Other Toxic Effects on Slightly hazardous in case of skin contact (irritant), of ingestion, of inhalation.
Humans
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on Not available.
Chronic Effects on Humans
Special Remarks on other Acute Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation.
Eyes: May cause eye irritation.
Inhalation: May cause respiratory tract irritation.
Ingestion: May cause gastrointestinal irritation or disturbances with nausea, vomiting, hypermotility,
diarrhea.. May affect behavior/central nervous system (tremor, ataxia, somnolence), respiration (dyspnea),
blood (leukopenia). It may also affect the liver.

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Section 12. Ecological Information
Ecotoxicity Not available.
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 less toxic than the product itself.
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

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Section 13. Disposal Considerations
Waste Disposal Waste must be disposed of in accordance with federal, state and local environmental
control regulations.

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Identification Not applicable.
Special Provisions for Not applicable.
Transport
DOT (Pictograms)
Fusidic Acid Sodium Salt

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Section 15. Other Regulatory Information and Pictograms
No products were found.
Federal and State
Regulations
California California prop. 65: This product contains the following ingredients for which the State of California has
Proposition 65 found to cause cancer which would require a warning under the statute: No products were found.
Warnings
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: No products were found.
Other Regulations EINECS: This product is on the European Inventory of Existing Commercial Chemical Substances (EINECS
No. 212-030-3).
Canada: Listed on Canadian Domestic Substance List (DSL).
China: Not listed on National Inventory.
Japan: Not listed on National Inventory (ENCS).
Korea: Not listed on National Inventory (KECI).
Philippines: Not listed on National Inventory (PICCS).
Australia: Listed on AICS.
Other Classifications WHMIS (Canada) Not controlled under WHMIS (Canada).
DSCL (EEC) R22- Harmful if swallowed. S46- If swallowed, seek medical advice
immediately and show this container or label.
Health Hazard
HMIS (U.S.A.) 1 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
1 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.
Fusidic Acid Sodium Salt

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

窄谱抗生素——夫西地酸钠

概述 夫西地酸钠，又称为褐霉酸钠或梭链孢酸钠，是一种甾体骨架结构的窄谱抗生素。由丹麦利奥制药公司首次研发成功，商品名为立思丁。它具有较强的组织渗透力，在肝脏内代谢，并通过胆汁排泄，几乎不经过肾脏排出。夫西地酸钠主要通过抑制细菌蛋白质合成产生杀菌作用，对革兰阳性菌表现出良好的抗菌效果。此外，它还对青霉素、甲氧西林等抗生素耐药的菌株敏感，且与临床使用的其他抗菌药物之间无交叉耐药性。

药理作用 夫西地酸钠主要应用于治疗由各种敏感细菌（特别是葡萄球菌）引起的各种感染，如骨髓炎、败血症、心内膜炎、反复感染的囊性纤维化、肺炎、脑膜炎、白喉、结核病以及皮肤和软组织感染。静脉给药适用于严重感染或耐药菌株感染，尤其是MRSA感染。口服治疗难辨梭状芽孢杆菌所致伪膜性肠炎效果显著。

药代动力学 夫西地酸钠主要作用于细菌的核糖体，通过抑制mRNA位移来阻断蛋白合成从而产生杀菌作用。口服后吸收良好，单剂0.5g口服2小时后的血药浓度为14～38mg/L，每日3次，第4日血药浓度可达21～71mg/L。药物无积蓄性，进食可影响其吸收。静脉滴注0.5g后2小时的血药浓度为40mg/L。该药物具有高脂溶性和良好的组织渗透能力，可透入房水、前列腺、滑囊液等有效部位，并能顺利透过胎盘屏障。夫西地酸钠主要在肝脏代谢，通过胆汁排出，几乎不经过肾脏排泄。

不良反应与注意事项 口服可能引起轻微胃肠道不适；静脉注射可能会导致血栓性静脉炎和静脉痉挛。大剂量静脉给药可能导致可逆性转氨酶升高及个别病人出现可逆黄疸现象。尽管罕见，但仍需注意过敏反应的可能性。对肝功能不全或胆道异常的患者，建议定期检查肝功能。

生物活性 Fusidate Sodium（立思丁）是fusidic acid的钠盐形式，用于局部治疗皮肤感染，具有抗菌作用，特别是针对革兰阳性菌和奈瑟球菌、结核杆菌。研究显示，Fusidin可通过抑制TNF-a分泌改善实验性自身免疫性心肌炎，并能减弱经streptozotocin处理后小鼠的免疫炎症糖尿病特征。

用途 夫西地酸钠主要用于治疗革兰阳性菌感染及奈瑟球菌、结核杆菌引起的感染。其抗菌谱广泛，对青霉素、甲氧西林和其它抗菌素耐药的菌株高度敏感，并且与其他临床使用的抗生素之间无交叉耐药性。通常用于皮肤骨组织及关节等部位感染以及心内膜炎治疗。

包装 25公斤纸板桶。

反应信息

• 作为反应物：
  描述：

  fusidic acid sodium salt 在 溶剂黄146 作用下， 以 水 为溶剂， 生成 夫西地酸
  参考文献：
  名称：

  秀丽线虫的梭链孢酸环B羟基化

  摘要：

  研究了利用线虫Cunninghamella elegans NRRL 1392进行梭链孢酸（1）的生物转化。夫西地酸（二羟基化衍生物2，3）中分离，并使用各种光谱技术，包括1D，2D NMR和HRESI-FTMS被完全阐明其结构。秀丽线虫NRRL 1392介导环B的羟基化以产生7-β-羟基（化合物2）和6-β-羟基夫西地酸（化合物3）。评估了化合物2和3对不同革兰氏阳性和-阴性细菌以及耻垢分枝杆菌的抗菌活性。与夫西地酸相比，B环羟基化导致活性降低。对于在最低能量之一的10kcal / mol内的所有构象异构体，计算了环B和C-3和C-16官能团的羟基化位点之间的平均距离。

  DOI：

  10.1016/j.phytol.2018.04.003

文献信息

• [EN] NITROGEN RING CONTAINING COMPOUNDS FOR TREATMENT OF INFLAMMATORY DISORDERS<br/>[FR] COMPOSÉS CONTENANT UN CYCLE AZOTÉ POUR LE TRAITEMENT DE TROUBLES INFLAMMATOIRES
  申请人：WEINGARTEN M DAVID

  公开号：WO2012135669A1

  公开（公告）日：2012-10-04

  The invention provides compounds, pharmaceutical compositions and methods of treatment of inflammatory disorders including a compound of Formula I, or its pharmaceutically acceptable salt, ester, pharmaceutically acceptable derivative or prodrug wherein R1, R2, R3, R4, X, Y, W, Z and Q are as defined herein.

  这项发明提供了化合物、药物组合物和治疗炎症性疾病的方法，包括式I的化合物，或其药用可接受的盐、酯、药用可接受的衍生物或前药，其中R1、R2、R3、R4、X、Y、W、Z和Q如本文所定义。
• [EN] COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS<br/>[FR] COMPOSÉS DESTINÉS AU TRAITEMENT DE TROUBLES MÉDICAUX
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2017035360A1

  公开（公告）日：2017-03-02

  Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula (I), or a pharmaceutically acceptable salt or composition thereof The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

  化合物、使用方法和制备抑制补体因子D的方法，包括式（I）的药用盐或其组合物。本文描述的抑制剂针对因子D并抑制或调节补体级联反应。本文描述的因子D的抑制剂减少了过度激活的补体。
• [EN] ALKYNE COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS<br/>[FR] COMPOSÉS ALCYNE POUR LE TRAITEMENT DE TROUBLES IMMUNITAIRES ET INFLAMMATOIRES
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2017035415A1

  公开（公告）日：2017-03-02

  Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

  提供含有公式I、I"和I'"的补体因子D抑制剂、使用方法和制备过程，或其药物可接受的盐或组合物。本文所述的抑制剂针对因子D并抑制或调节补体级联反应。本文所述的因子D抑制剂减少了补体的过度激活。
• [EN] ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS<br/>[FR] COMPOSÉS ARYLE, HÉTÉROARYLE, ET HÉTÉROCYCLIQUES POUR LE TRAITEMENT DE TROUBLES IMMUNITAIRES ET INFLAMMATOIRES
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2017035409A1

  公开（公告）日：2017-03-02

  Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

  提供含有公式I、I"和I'"的补体因子D抑制剂、使用方法和制备过程，或其药物可接受的盐或组合物。本文所述的抑制剂针对因子D并抑制或调节补体级联反应。本文所述的因子D抑制剂减少了补体的过度激活。
• [EN] MACROCYCLIC COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS<br/>[FR] COMPOSÉS MACROCYCLIQUES DESTINÉS AU TRAITEMENT DE TROUBLES MÉDICAUX
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2018160892A1

  公开（公告）日：2018-09-07

  Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

  提供大环补体因子D抑制剂、药物组合物及其用途，以及它们的制造工艺。所提供的化合物包括公式I、公式II、公式III、公式IV、公式V、公式VI、公式VII和公式VIII或其药用可接受的盐、前药、同位素类似物、N-氧化物或孤立的同分异构体，可选地存在于药用可接受的组合物中。此处描述的抑制剂针对因子D并抑制或调节补体级联反应。