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| 中文名 | 雷西莫特 |
|---|---|
| 英文名 | resiquimod |
| 中文别名 |
瑞喹莫德
4-氨基-2-乙氧基甲基-ALPHA,ALPHA-二甲基-1H-咪唑并[4,5-C]喹啉-1-乙醇 1-(4-氨基-2-(乙氧基甲基)-1H-咪唑并[4,5-C]喹啉-1-基)-2-甲基-2-丙醇 |
| 英文别名 |
1-[4-Amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-2-methyl-2-propanol
1H-imidazo[4,5-c]quinoline-1-ethanol, 4-amino-2-(ethoxymethyl)-α,α-dimethyl- Resiquimod 1-[4-amino-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol 1-(4-Amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl)-2-methylpropan-2-ol 4-amino-2-(ethoxymethyl)-a,a-dimethyl-1h-imidazo[4,5-c]quinoline-1-ethanol 1-[4-Amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-ol R848 |
| 描述 | Resiquimod是一种Toll样受体7和8 (TLR7/TLR8) 的激动剂, 诱导细胞因子如TNF-α,IL-6和IFN-α的上调。 |
|---|---|
| 相关类别 | |
| 体外研究 | Resiquimod(R-848)诱导半抗原和过敏原特异性循环T细胞,包括TH2效应子,产生IFN-γ,甚至丧失产生IL-4的能力[2]。 Resiquimod(R848)以剂量依赖性方式增强PBL增殖,并增加BrdU掺入测定中BrdU阳性细胞的数量。用R848处理的细胞显示出显着增加的(3.5倍)荧光素酶(NF-κB活性的报道基因)活性[3]。 |
| 体内研究 | Resiquimod(R-848)(50μg/只,im途径)显着上调SPF中IFN-α,IFN-β,IFN-γ,IL-1β,IL-4,iNOS和MHC-II基因的表达鸡[1]。 |
| 激酶实验 | 对于荧光素酶测定，用萤火虫NF-κB特异性荧光素酶报告载体pNFκB-Met-Luc2转染FG-9307细胞。通过与pSEAP2对照载体共转染来监测转染效率，所述pSEAP2对照载体组成型表达人分泌的增强的碱性磷酸酶（SEAP）。然后用Resiquimod（R848,1μg/ mL），CQ（10μM），CQ加R848或PBS处理细胞，并在22℃温育24小时。然后分别使用荧光素酶测定试剂盒和Great EscAPe TM SEAP化学发光检测试剂盒分析转染子的培养基的荧光素酶活性和SEAP活性。该测定进行三次。 |
| 细胞实验 | 为了抑制溶酶体酸化，在Resiquimod（R848）处理之前将细胞与10μMSQ一起温育1小时。处理后，向板中加入20μL5mg/ mL MTT。将板在22℃温育4小时，并向板中加入200μL二甲基亚砜以溶解还原的甲..然后用酶标仪在490nm处读板。为了确定Myd88抑制对R848诱导的细胞增殖的影响，将Myd88抑制剂Pepinh-MYD和对照肽Pepinh-Control以50μM的浓度加入PBL中，并将板在22℃温育6小时。 。温育后，用R848处理细胞，并如上进行MTT测定。为了确定NF-κB失活对R848诱导的细胞增殖的影响，将BAY-11-7082（IκB-α磷酸化的不可逆抑制剂）以1μM的浓度添加到细胞中，并将板在22℃温育。 °C 1小时。温育后，用R848处理细胞，并如前所述进行MTT测定。所有实验均进行三次。 |
| 动物实验 | 将总共40只两周龄的SPF鸡分配给以下四个实验组之一（n = 10 /组）：组A：PBS对照; B组：灭活的NDV疫苗; C组：由lentogenic菌株和D组制备的商业油佐剂灭活的NDV疫苗：灭活的NDV疫苗和R-848（50μg/禽）的组合。通过肌肉途径在大腿肌肉中施用疫苗或PBS。免疫后14天（dpi）给予加强剂量。在加强免疫后两周，实验性SPF禽类用肌肉注射NDV（每只鸡105只ELD50）的速发菌株进行攻击。每天观察临床症状和死亡率直至攻击后14天（dpc）。在攻击后第0,4,7和14天从鸟类收集阴沟拭子（n = 6 /组），并通过尿囊内途径接种到10日龄的含胚鸡蛋（n = 3个卵/样品）中。接种后3天，使用10％鸡RBC通过斑点血细胞凝集检查尿囊液的NDV生长。 |
| 参考文献 |
| 密度 | 1.3±0.1 g/cm3 |
|---|---|
| 沸点 | 553.6±50.0 °C at 760 mmHg |
| 熔点 | 193 °C |
| 分子式 | C17H22N4O2 |
| 分子量 | 314.382 |
| 闪点 | 288.6±30.1 °C |
| 精确质量 | 314.174286 |
| PSA | 86.19000 |
| LogP | 2.15 |
| 外观性状 | 固体;White to Light yellow to Light orange powder to crystal |
| 蒸汽压 | 0.0±1.6 mmHg at 25°C |
| 折射率 | 1.635 |
| 储存条件 | -20°C;存放于惰性气体之中;避免湿气 (吸湿),加热 |
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SECTION 1: Identification of the substance/mixture and of the company/undertaking Product identifiers Product name: Resiquimod : SML0196 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.: 144875-48-9 SECTION 2: Hazards identification Classification of the substance or mixture Not a hazardous substance or mixture according to Regulation (EC) No. 1272/2008. Not a hazardous substance or mixture according to EC-directives 67/548/EEC or 1999/45/EC. Label elements The product does not need to be labelled in accordance with EC directives or respective national laws. Other hazards - none SECTION 3: Composition/information on ingredients Substances Synonyms: 4-Amino-2-(ethoxymethyl)-alpha,alpha-dimethyl-1H-imidazo(4,5- c)quinoline-1-ethanol R-848 Formula: C17H22N4O2 Molecular Weight: 314,38 g/mol CAS-No.: 144875-48-9 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 no data available 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 Hygroscopic. Store with desiccant. Specific end use(s) A part 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 The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and the standard EN 374 derived from it. 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. 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: powder b) Odourno data available c) Odour Thresholdno data available d) pH7,2 e) Melting point/freezing166 °C 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 solubilityno data available o) Partition coefficient: n- log Pow: 2,109 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 no data available 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 Biochemical:Metabolism (intermediary): Effect on inflammation or mediation of inflammation. 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: NJ5911320 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 SECTION 16 - ADDITIONAL INFORMATION N/A |
| 危险品运输编码 | NONH for all modes of transport |
|---|---|
| RTECS号 | NJ5911320 |
| 海关编码 | 2933990090 |
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| 文献：US6348462 B1, ; Page column 33, 34 ; |
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| 文献：ASCEND BIOPHARMACEUTICALS PTY LTD; PIETERSZ, Geoffrey, Alan Patent: WO2013/67597 A1, 2013 ; Location in patent: Page/Page column 80 ; |
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| 文献：WO2013/67597 A1, ; |
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| 上游产品 7 | |
|---|---|
| 下游产品 1 | |
| 海关编码 | 2933990090 |
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| 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% |
