179463-17-3

• 常用中文名：醋酸卡泊芬净
• 常用英文名：Cancidas
• CAS号：179463-17-3
• 分子式：C₅₆H₉₆N₁₀O₁₉
• 分子量：1093.31000
• 相关类别： 原料药 专科用药 眼科用药
• 发布时间：2018-07-26 07:13:51
• 更新时间：2024-01-02 09:47:06
• Caspofungin Acetate 是一种抗真菌药,能够非竞争性地抑制1,3-β-d葡聚糖合酶的合成。

名称

• 中文名: 醋酸卡泊芬净
• 英文名: caspofungin acetate
• 英文别名: Mk0991; L-743,872; CASPOFUNGIN; Cancidas; Tetradecanamide, N-[(2R,6S,9S,11R,12S,14aS,15S,20S,23S,25aS)-12-[(2-aminoethyl)amino]-20-[(1R)-3-amino-1-hydroxypropyl]-23-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]tetracosahydro-2,11,15-trihydroxy-6-[(1R)-1-hydroxyethyl]-5,8,14,19,22,25-hexaoxo-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacycloheneicosin-9-yl]-10,12-dimethyl-, acetate (1:2) (salt); N-{(2R,6S,9S,11R,12S,14aS,15S,20S,23S,25aS)-12-[(2-Aminoethyl)amino]-20-[(1R)-3-amino-1-hydroxypropyl]-23-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-2,11,15-trihydroxy-6-[(1R)-1-hydroxyethyl]-5,8,14,19,22,25-hexaoxotetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosin-9-yl}-10,12-dimethyltetradecanamide acetate (1:2); Caspofungin Diacetate; Caspofungin (Acetate)

物化性质

• 沸点: 1408.1ºC at 760 mmHg
• 分子式: C₅₆H₉₆N₁₀O₁₉
• 分子量: 1093.31000
• 精确质量: 1092.64000
• PSA: 412.03000
• LogP: 0.06150
• 外观性状: white to beige
• 蒸汽压: 0mmHg at 25°C
• 储存条件: ?20°C
• 水溶解性: H2O: soluble15mg/mL (clear solution)

生物活性

• 描述: Caspofungin Acetate 是一种抗真菌药,能够非竞争性地抑制1,3-β-d葡聚糖合酶的合成。
• 相关类别:
  信号通路 >> 抗感染 >> 真菌
  研究领域 >> 感染
• 体内研究: 注射卡泊芬净的小鼠在0.41至4.1μM的玻璃体浓度下,其ERG波形没有显着改变,并且它们的视网膜没有可检测的形态变化或细胞损失。在41μM的玻璃体浓度下,卡泊芬净降低了ERG的a波,b波和暗视阈值响应的幅度,并且还导致神经节细胞层中细胞数量的减少[1]。卡普芬净(8 mg/kg)或两性霉素B 1 mg/kg,感染后30 h每天一次腹膜内注射,连续7天,相对于媒介物对照治疗,第28天100％存活,导致白天100％死亡率11,传染性挑战后。与第5天的媒介物对照治疗相比,当控制负荷达到峰值时,卡泊芬净降低了肾和脑组织中存活念珠菌的恢复。给予2mg/kg或更高剂量的卡泊芬净治疗的小鼠在第5天具有比两性霉素B治疗的小鼠显着更低的脑负荷。两性霉素B和卡泊芬净治疗使肾脏真菌负荷减少1.7log CFU/g和2.46至3.64log CFU/g,分别为[2]。
• 动物实验: 在感染性攻击后30小时开始抗真菌治疗，并通过腹膜内（ip）注射每天一次给予7天。用1,2,4或8mg / kg /天的卡泊芬净，1mg / kg /天的两性霉素B或载体对照（无菌蒸馏水）处理小鼠。通过3种方式评估该模型的功效：通过监测每个治疗组中10只动物的存活率，通过监测第二组治疗动物的肾和脑组织中的念珠菌负荷，以及通过组织学评估其中的肾和脑。第三组治疗动物。通过CO 2吸入使小鼠安乐死，并且在30小时（仅媒介物处理的对照）和第5天（第4剂量后24小时），8（最后一次剂量后24小时），14,21小时对培养和组织学的组织取样。 （仅卡泊芬净处理），和攻击后28。
• 参考文献:

  [1]. Mojumder DK, et al. Evaluating retinal toxicity of intravitreal caspofungin in the mouse eye. Invest Ophthalmol Vis Sci. 2010 Nov;51(11):5796-803.

  [2]. Flattery, Amy M. et al. Efficacy of caspofungin in a juvenile mouse model of central nervous system candidiasis. Antimicrobial Agents and Chemotherapy (2011), 55(7), 3491-3497.

MSDS

SECTION 1: Identification of the substance/mixture and of the company/undertaking Product identifiers Product name: Caspofungin diacetate REACH No.: A registration number is not available for this substance as the substance or its uses are exempted from registration, the annual tonnage does not require a registration or the registration is envisaged for a later registration deadline. CAS-No.: 179463-17-3 Relevant identified uses of the substance or mixture and uses advised against Identified uses: Laboratory chemicals, Manufacture of substances SECTION 2: Hazards identification Classification of the substance or mixture Not a hazardous substance or mixture according to Regulation (EC) No. 1272/2008. This substance is not classified as dangerous according to Directive 67/548/EEC. Label elements This substance is not classified as dangerous according to Directive 67/548/EEC. Other hazards - none SECTION 3: Composition/information on ingredients Substances Formula: C52H88N10O15 . 2C2H4O2 Molecular Weight: 1.213,42 g/mol CAS-No.: 179463-17-3 No components need to be disclosed according to the applicable regulations. SECTION 4: First aid measures Description of first aid measures If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. In case of skin contact Wash off with soap and plenty of water. In case of eye contact Flush eyes with water as a precaution. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Most important symptoms and effects, both acute and delayed The most important known symptoms and effects are described in the labelling (see section 2.2) and/or in section 11 Indication of any immediate medical attention and special treatment needed no data available SECTION 5: Firefighting measures Extinguishing media Suitable extinguishing media Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide. Special hazards arising from the substance or mixture Carbon oxides, nitrogen oxides (NOx) Advice for firefighters Wear self contained breathing apparatus for fire fighting if necessary. Further information no data available SECTION 6: Accidental release measures Personal precautions, protective equipment and emergency procedures Avoid dust formation. Avoid breathing vapours, mist or gas. For personal protection see section 8. Environmental precautions Do not let product enter drains. Methods and materials for containment and cleaning up Sweep up and shovel. Keep in suitable, closed containers for disposal. Reference to other sections For disposal see section 13. SECTION 7: Handling and storage Precautions for safe handling Provide appropriate exhaust ventilation at places where dust is formed. For precautions see section 2.2. Conditions for safe storage, including any incompatibilities Store in cool place. Keep container tightly closed in a dry and well-ventilated place. Recommended storage temperature: -20 °C Specific end use(s) Apart from the uses mentioned in section 1.2 no other specific uses are stipulated SECTION 8: Exposure controls/personal protection Control parameters Components with workplace control parameters Exposure controls Appropriate engineering controls General industrial hygiene practice. Personal protective equipment Eye/face protection Use equipment for eye protection tested and approved under appropriate government standards such as NIOSH (US) or EN 166(EU). Skin protection Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique (without touching glove's outer surface) to avoid skin contact with this product. Dispose of contaminated gloves after use in accordance with applicable laws and good laboratory practices. Wash and dry hands. The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. Body Protection Choose body protection in relation to its type, to the concentration and amount of dangerous substances, and to the specific work-place., The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Respiratory protection Respiratory protection is not required. Where protection from nuisance levels of dusts are desired, use type N95 (US) or type P1 (EN 143) dust masks. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). Control of environmental exposure Do not let product enter drains. SECTION 9: Physical and chemical properties Information on basic physical and chemical properties a) AppearanceForm: solid b) Odourno data available c) Odour Thresholdno data available d) pHno data available e) Melting point/freezingno data available point f) Initial boiling point and no data available boiling range g) Flash pointno data available h) Evapouration rateno data available i) Flammability (solid, gas) no data available j) Upper/lowerno data available flammability or explosive limits k) Vapour pressureno data available l) Vapour densityno data available m) Relative densityno data available n) Water solubility0,028 g/l at 25 °C o) Partition coefficient: n- no data available octanol/water p) Auto-ignitionno data available temperature q) Decompositionno data available temperature r) Viscosityno data available s) Explosive propertiesno data available t) Oxidizing propertiesno data available Other safety information Solubility in otherMethanol - soluble solvents SECTION 10: Stability and reactivity Reactivity no data available Chemical stability Stable under recommended storage conditions. Possibility of hazardous reactions no data available Conditions to avoid no data available Incompatible materials Strong oxidizing agents Hazardous decomposition products Other decomposition products - no data available In the event of fire: see section 5 SECTION 11: Toxicological information Information on toxicological effects Acute toxicity no data available Skin corrosion/irritation no data available Serious eye damage/eye irritation no data available Respiratory or skin sensitisation no data available Germ cell mutagenicity no data available Carcinogenicity IARC:No component of this product present at levels greater than or equal to 0.1% is identified as probable, possible or confirmed human carcinogen by IARC. Reproductive toxicity no data available Specific target organ toxicity - single exposure no data available Specific target organ toxicity - repeated exposure no data available Aspiration hazard no data available Additional Information RTECS: TP8046500 Liver, To the best of our knowledge, the chemical, physical, and toxicological properties have not been thoroughly investigated. SECTION 12: Ecological information Toxicity no data available Persistence and degradability no data available Bioaccumulative potential no data available Mobility in soil no data available Results of PBT and vPvB assessment PBT/vPvB assessment not available as chemical safety assessment not required/not conducted Other adverse effects no data available SECTION 13: Disposal considerations Waste treatment methods Product Offer surplus and non-recyclable solutions to a licensed disposal company. Contaminated packaging Dispose of as unused product. SECTION 14: Transport information UN number ADR/RID: -IMDG: -IATA: - UN proper shipping name ADR/RID: Not dangerous goods IMDG: Not dangerous goods IATA:Not dangerous goods Transport hazard class(es) ADR/RID: -IMDG: -IATA: - Packaging group ADR/RID: -IMDG: -IATA: - Environmental hazards ADR/RID: noIMDG Marine pollutant: noIATA: no Special precautions for user no data available SECTION 15: Regulatory information This safety datasheet complies with the requirements of Regulation (EC) No. 1907/2006. Safety, health and environmental regulations/legislation specific for the substance or mixture no data available Chemical Safety Assessment For this product a chemical safety assessment was not carried out SECTION 16: Other information Further information Copyright 2014 Co. LLC. License granted to make unlimited paper copies for internal use only. The above information is believed to be correct but does not purport to be all inclusive and shall be used only as a guide. The information in this document is based on the present state of our knowledge and is applicable to the product with regard to appropriate safety precautions. It does not represent any guarantee of the properties of the product. Corporation and its Affiliates shall not be held liable for any damage resulting from handling or from contact with the above product. See and/or the reverse side of invoice or packing slip for additional terms and conditions of sale.

安全

• 危险品运输编码: NONH for all modes of transport
• RTECS号: TP8046500
• 海关编码: 2933990090

海关

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%