7421-40-1

• 常用中文名：甘珀酸钠
• 常用英文名：Carbenoxolone disodium
• CAS号：7421-40-1
• 分子式：C₃₄H₄₈Na₂O₇
• 分子量：614.72000
• 相关类别： 原料药 消化系统用药 抗酸及胃黏膜保护药
• 发布时间：2018-08-04 21:32:47
• 更新时间：2024-01-08 11:54:50
• Carbenoxolone disodium 是甘草酸 (HY-N0184) 的活性代谢物和人 11β-HSD 和细菌 3α, 20β-HSD 的抑制剂。Carbenoxolone disodium 是一种缝隙连接的解耦剂 (gap junctions) 和并且可以有效抑制牛痘病毒生长。Carbenoxolone disodium 可用于研究消化性、食道和口腔溃疡和炎症的相关研究。

名称

• 中文名: 甘珀酸钠
• 英文名: Carbenoxolone disodium,(3β,20β)-3-(3-Carboxy-1-oxopropoxy)-11-oxoolean-12-en-29-oicaciddisodium
• 中文别名: 氢琥珀酸甘草次酸; 18β-甘草次酸半琥珀酸酯二钠; 氢琥珀酸甘草次酸二钠盐
• 英文别名: sodium carbenoxolone; pyrogastrone; CARBENOXOLONE SODIUM; EINECS 231-044-0; ulcus-tablinen; neogel; sanodin; Carbenoxolon-Dinatriumsalz; duogastrone; Carbenoxalone Sodium; carbenoxolone disodium; Biogastrone; MFCD00079043

物化性质

• 沸点: 687.4ºC at 760 mmHg
• 分子式: C₃₄H₄₈Na₂O₇
• 分子量: 614.72000
• 闪点: 211.6ºC
• 精确质量: 614.32000
• PSA: 123.63000
• LogP: 4.15890
• 储存条件: 库房低温通风干燥

生物活性

• 描述: Carbenoxolone disodium 是甘草酸 (HY-N0184) 的活性代谢物和人 11β-HSD 和细菌 3α, 20β-HSD 的抑制剂。Carbenoxolone disodium 是一种缝隙连接的解耦剂 (gap junctions) 和并且可以有效抑制牛痘病毒生长。Carbenoxolone disodium 可用于研究消化性、食道和口腔溃疡和炎症的相关研究。
• 相关类别:
  研究领域 >> 感染
  研究领域 >> 炎症/免疫
  信号通路 >> 细胞骨架 >> 间隙连接蛋白
• 靶点:

  IC50: human 11β-HSD; bacterial 3α, 20β-HSD[1]; gap junction; Vaccinia virus[2]

• 体外研究: 卡宾诺酮二钠(6-150μM；预处理1小时)抑制痘苗病毒(VACV)在一个独立于HaCaT细胞的缝隙连接中的复制,并且在48小时对VACV-A5L-EGFP感染细胞具有毒性作用[2]。卡宾诺酮(30μM；预处理1小时)不上调PP2A的表达,但诱导hacat细胞中晚期蛋白A27的表达[2]。细胞活力测定[2]细胞系：HaCaT细胞浓度：6μM、12μM、30μM、60μM、150μM孵育时间：预处理1小时结果：病毒感染细胞在高剂量下48小时前无毒性。Western Blot分析[2]细胞系：HaCaT细胞浓度：30μM孵育时间：预处理1h结果：A27表达明显上调。
• 体内研究: 卡宾索酮(腹腔注射；100、200和300 mg/kg；地西泮前30、60和60 min)不诱导肌肉松弛剂活性,与生理盐水相比显示出肌肉松弛剂活性,并且在牵引试验中这种作用比地西泮更大[3]。在戊四氮(PTZ)癫痫模型中,卡宾诺酮(腹腔注射,100、200和300mg/kg,戊四氮前30、60和60min)显著增加小鼠睡眠时间,降低潜伏期。ED50值为83.3 mg/kg(%95 CL:556.29)[3]。动物模型：雄性BALB/c小鼠[3]剂量：100、200、300mg/kg给药：腹腔注射；戊四唑前30、60、60min结果：小鼠睡眠时间明显延长。
• 参考文献:

  [1]. W L Duax, et al. Steroid Dehydrogenase Structures, Mechanism of Action, and Disease. Vitam Horm. 2000;58:121-48.

  [2]. Hossein Hosseinzadeh, et al. Anticonvulsant, Sedative and Muscle Relaxant Effects of Carbenoxolone in Mice. BMC Pharmacol. 2003 Apr 29;3:3.

  [3]. Ismar R Haga, et al. Carbenoxolone-mediated Cytotoxicity Inhibits Vaccinia Virus Replication in a Human Keratinocyte Cell Line. Sci Rep. 2018 Nov 16;8(1):16956.

MSDS

Section1. IDENTIFICATION OF THE SUBSTANCE/MIXTURE Product identifiers Product name: Carbenoxolone disodium salt CAS-No.: 7421-40-1 Relevant identified uses of the substance or mixture and uses advised against Identified uses: Laboratory chemicals, Manufacture of substances Section2. HAZARDS IDENTIFICATION Classification of the substance or mixture Classification according to Regulation (EC) No 1272/2008 [EU-GHS/CLP] Eye irritation (Category 2) Classification according to EU Directives 67/548/EEC or 1999/45/EC Irritating to eyes. Label elements Labelling according Regulation (EC) No 1272/2008 [CLP] Pictogram Signal wordWarning Hazard statement(s) H319Causes serious eye irritation. Precautionary statement(s) P305 + P351 + P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. Supplemental Hazardnone Statements According to European Directive 67/548/EEC as amended. Hazard symbol(s) R-phrase(s) R36Irritating to eyes. S-phrase(s) S26In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36Wear suitable protective clothing. Other hazards - none Section3. COMPOSITION/INFORMATION ON INGREDIENTS Substances : 3β-Hydroxy-11-oxoolean-12-en-30-oic acid 3-hemisuccinate Synonyms Formula: C34H48Na2O7 Molecular Weight: 614,72 g/mol ComponentConcentration Carbenoxolone disodium CAS-No.7421-40-1- EC-No.231-044-0 Section4. FIRST AID MEASURES Description of first aid measures General advice Consult a physician. Show this safety data sheet to the doctor in attendance. If inhaled If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician. In case of skin contact Wash off with soap and plenty of water. Consult a physician. In case of eye contact Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician. If swallowed Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician. Most important symptoms and effects, both acute and delayed To the best of our knowledge, the chemical, physical, and toxicological properties have not been thoroughly investigated. Indication of any immediate medical attention and special treatment needed no data available Section5. 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, Sodium oxides Advice for firefighters Wear self contained breathing apparatus for fire fighting if necessary. Further information no data available Section6. ACCIDENTAL RELEASE MEASURES Personal precautions, protective equipment and emergency procedures Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure adequate ventilation. Avoid breathing dust. Environmental precautions Do not let product enter drains. Methods and materials for containment and cleaning up Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed containers for disposal. Reference to other sections For disposal see section 13. Section7. HANDLING AND STORAGE Precautions for safe handling Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed. 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: 2 - 8 °C Specific end uses no data available Section8. EXPOSURE CONTROLS/PERSONAL PROTECTION Control parameters Components with workplace control parameters Exposure controls Appropriate engineering controls Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and at the end of workday. Personal protective equipment Eye/face protection Safety glasses with side-shields conforming to EN166 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 impervious clothing, The type of protective equipment must be selected according to the concentration and amount of the dangerous substance at the specific workplace. Respiratory protection For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges. Use respirators and components tested and approved under appropriate government standards such as NIOSH (US) or CEN (EU). Section9. 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) Evaporation 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- no data available octanol/water p) Autoignitionno 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 Section10. STABILITY AND REACTIVITY Reactivity no data available Chemical stability no data available Possibility of hazardous reactions no data available Conditions to avoid no data available Incompatible materials no data available Hazardous decomposition products Other decomposition products - no data available Section11. TOXICOLOGICAL INFORMATION Information on toxicological effects Acute toxicity LD50 Oral - rat - 2.450 mg/kg Remarks: Cardiac:Pulse rate. Respiratory disorder Skin and Appendages: Other: Hair. Skin corrosion/irritation no data available Serious eye damage/eye irritation no data available Respiratory or skin sensitization 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 Potential health effects InhalationMay be harmful if inhaled. May cause respiratory tract irritation. IngestionMay be harmful if swallowed. SkinMay be harmful if absorbed through skin. May cause skin irritation. EyesCauses serious eye irritation. Signs and Symptoms of Exposure To the best of our knowledge, the chemical, physical, and toxicological properties have not been thoroughly investigated. Additional Information RTECS: RK0250000 Section12. 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 no data available Other adverse effects no data available Section13. DISPOSAL CONSIDERATIONS Waste treatment methods Product Offer surplus and non-recyclable solutions to a licensed disposal company. Dissolve or mix the material with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber. Contaminated packaging Dispose of as unused product. Section14. 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 Section15. 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 no data available Section16. OTHER INFORMATION Further information Copyright 2012 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.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RK0250000 CHEMICAL NAME : Olean-12-en-30-oic acid, 3-beta-hydroxy-11-oxo-, hydrogen succinate, disodium salt CAS REGISTRY NUMBER : 7421-40-1 LAST UPDATED : 199610 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C34-H48-O7.2Na MOLECULAR WEIGHT : 614.80 WISWESSER LINE NOTATION : T F6 E6 B666 DO BUTJ F1 IOV2VQ J1 J1 N1 O1 R1 U1VQ U1 &-NA- 2 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human DOSE/DURATION : 120 mg/kg/6W TOXIC EFFECTS : Vascular - BP elevation not characterized in autonomic section Nutritional and Gross Metabolic - changes in potassium REFERENCE : CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 117,1155,1977 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2450 mg/kg TOXIC EFFECTS : Cardiac - pulse rate Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 92 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FRMCE8 Farmaco. (Societa Chimica Italiana, Corso Strada Nova, 86, Casella Postale 227, 27100 Pavia, Italy) V.44- 1989- Volume(issue)/page/year: 49,281,1994 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1515 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 120 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 198 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 3900 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 371 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 1060 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 371 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 36400 mg/kg/26W-C TOXIC EFFECTS : Kidney, Ureter, Bladder - urine volume decreased Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,859,1976 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 12 gm/kg/30D-C TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in thymus weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,831,1976

安全

• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 22-36
• 安全声明 (欧洲): 26-36
• WGK德国: 3
• RTECS号: RK0250000