125-04-2

• 常用中文名：氢化可的松琥珀酸钠
• 常用英文名：Corlan
• CAS号：125-04-2
• 分子式：C₂₅H₃₃NaO₈
• 分子量：484.51
• 相关类别： 原料药 激素及调节内分泌功能类药 肾上腺皮质激素类药
• 发布时间：2018-02-04 08:00:00
• 更新时间：2024-01-09 12:23:39
• Hydrocortisone hemisuccinate sodium 是一种有口服活性的生理性糖皮质激素。Hydrocortisone hemisuccinate sodium 抑制 IL-6 和 IL-3 的生物活性,IC50 值分别为 6.7 和 21.4 μM。Hydrocortisone hemisuccinate sodium 可用于溃疡性结肠炎 (UC) 的研究。

名称

• 中文名: 氢化可的松琥珀酸钠
• 英文名: Hydrocortisone Hemisuccinate Sodium Salt
• 中文别名: 氢化可的松21-半琥珀酸钠盐; 皮質醇
• 英文别名: Pregn-4-ene-3,20-dione, 21-(3-carboxy-1-oxopropoxy)-11,17-dihydroxy-, monosodium salt, (11β)-; Sodium 4-{[(11β)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl]oxy}-4-oxobutanoate; Solu-Glyc; Butanedioic acid, mono[(11β)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl] ester, sodium salt (1:1); Hydrocortisone hemisuccinate sodium salt; Natrium-4-{2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy}-4-oxobutanoat; Intracort; Hydrocortisone sodium succinate; MFCD00069472; (11b)-21-(3-Carboxy-1-oxopropoxy)-11,17-dihydroxypregn-4-ene-3,20-dione Monosodium Salt; Saxizon; EINECS 204-725-5; Buccalsone; butanedioic acid, mono[(11β)-11,17-dihydroxy-3,20-dioxopregn-4-en-21-yl] ester, monosodium salt; Hydrocortisone 21-sodium succinate; Corlan; sodium 4-{2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-oxoethoxy}-4-oxobutanoate; Nordicort; 4-{2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-diméthyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tétradécahydro-1H-cyclopenta[a]phénanthrén-17-yl]-2-oxoéthoxy}-4-oxobutanoate de sodium; Sodium 17-hydroxycorticosterone 21-succinate

物化性质

• 沸点: 685.5ºC at 760mmHg
• 分子式: C₂₅H₃₃NaO₈
• 分子量: 484.51
• 闪点: 231.1ºC
• 精确质量: 484.207306
• PSA: 141.03000
• LogP: 0.86260
• 外观性状: powder
• 蒸汽压: 9.36E-22mmHg at 25°C
• 储存条件:

  −20℃。

• 水溶解性: H2O: 50 mg/mL
• 更多:

  1.性状：粉末。

  2.溶解度：H2O: 50 mg/mL。

生物活性

• 描述: Hydrocortisone hemisuccinate sodium 是一种有口服活性的生理性糖皮质激素。Hydrocortisone hemisuccinate sodium 抑制 IL-6 和 IL-3 的生物活性,IC50 值分别为 6.7 和 21.4 μM。Hydrocortisone hemisuccinate sodium 可用于溃疡性结肠炎 (UC) 的研究。
• 相关类别:
  研究领域 >> 代谢疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 糖皮质激素受体
• 体外研究: 半琥珀酸氢化可的松抑制IL-6和IL-3的生物活性,IC50分别为6.7和21.4μM,对IL-6非依赖性MH60细胞没有细胞毒性作用[3]。半琥珀酸氢化可的松钠(0.12-60μM；72小时)抑制外周淋巴细胞(PBL)和T淋巴细胞培养物中的植物血凝素(PHA)反应[3]。
• 体内研究: 半琥珀酸氢化可的松钠(30 mg/kg；每天两次,持续5天)可减少小鼠的体重减轻并增加食物摄入量[2]。动物模型：雄性Sprague-Dawley大鼠(200-220 g,10-11周)诱导结肠炎[2]剂量：30 mg/kg给药：每天两次,持续5天结果：与2,4,6-三硝基苯磺酸(TNBS)组相比,疾病活动指数(DAI)评分和髓过氧化物酶(MPO)活性显著降低。增加了体重。
• 参考文献:

  [1]. Kang BS, et, al. Inhibitory effects of anti-inflammatory drugs on interleukin-6 bioactivity. Biol Pharm Bull. 2001 Jun;24(6):701-3.

  [2]. You YC, et, al. In vitro and in vivo application of pH-sensitive colon-targeting polysaccharide hydrogel used for ulcerative colitis therapy. Carbohydr Polym. 2015 Oct 5;130:243-53.

  [3]. Langhoff E, et, al. The immunosuppressive potency in vitro of physiological and synthetic steroids on lymphocyte cultures. Int J Immunopharmacol. 1987;9(4):469-73.

MSDS

Section 1. Chemical Product and Company Identification Hydrocortisone Sodium SuccinateCatalog Common Name/ Number(s). Trade Name CAS#125-04-2 Manufacturer Commercial Name(s) Hydrocortisone Sodium Succinate Section 3. Hazards Identification Potential Acute Health Effects Slightly hazardous in case of skin contact (irritant), of eye contact (irritant), of ingestion, of inhalation. Potential Chronic HealthCARCINOGENIC EFFECTS: Not available. EffectsMUTAGENIC EFFECTS: Not available. TERATOGENIC EFFECTS: Not available. DEVELOPMENTAL TOXICITY: Not available. Repeated or prolonged exposure is not known to aggravate medical condition. Section 4. First Aid Measures Eye ContactCheck 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 ContactWash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation develops. Cold water may be used. Serious Skin ContactNot available. InhalationIf inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical attention. Serious InhalationNot available. IngestionDo 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 IngestionNot available. Section 5. Fire and Explosion Data Flammability of the Product May be combustible at high temperature. Auto-Ignition Temperature Not available. Flash PointsNot available. Flammable LimitsNot available. These products are carbon oxides (CO, CO2). Some metallic oxides. Products of Combustion Fire Hazards in Presence of Slightly flammable to flammable in presence of heat. Various Substances Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available. of Various SubstancesRisks of explosion of the product in presence of static discharge: Not available. Fire Fighting MediaSMALL FIRE: Use DRY chemical powder. and InstructionsLARGE FIRE: Use water spray, fog or foam. Do not use water jet. Special Remarks onAs with most organic solids, fire is possible at elevated temperatures. Fire HazardsMaterial in powder form, capable of creating a dust explosion. Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presence of an ignition source is a potential dust Hazardsexplosion hazard. Hydrocortisone Sodium Succinate Section 6. Accidental Release Measures Small SpillUse 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 SpillUse 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. Section 7. Handling and Storage PrecautionsKeep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not breathe dust. Keep away from incompatibles such as oxidizing agents. StorageKeep container tightly closed. Keep container in a cool, well-ventilated area. Do not store above -20°C (-4°F). Freeze. Section 8. Exposure Controls/Personal Protection Engineering ControlsUse 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 ProtectionSafety 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 used a Large Spillto avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist BEFORE handling this product. Exposure LimitsNot available. Section 9. Physical and Chemical Properties Physical state and appearance Solid. (Powdered solid.)OdorNot available. TasteNot available. Molecular Weight484.52 g/mole White. Off-white. Color Not available. pH (1% soln/water) Boiling PointNot available. Not available. Melting Point Critical TemperatureNot available. Specific GravityNot available. Vapor PressureNot applicable. Vapor DensityNot available. VolatilityNot available. Odor ThresholdNot available. Water/Oil Dist. Coeff.Not available. Ionicity (in Water)Not available. Dispersion PropertiesSee solubility in water. SolubilitySoluble in cold water. Hydrocortisone Sodium Succinate Section 10. Stability and Reactivity Data The product is stable. Stability Instability TemperatureNot available. Excess heat, incompatible materials, moisture Conditions of Instability Reactive with oxidizing agents. Incompatibility with various substances CorrosivityNot available. Special Remarks onNot available. Reactivity Special Remarks onNot available. Corrosivity PolymerizationWill not occur. Section 11. Toxicological Information Routes of EntryInhalation. Ingestion. Toxicity to AnimalsLD50: Not available. LC50: Not available. Chronic Effects on Humans Not available. Other Toxic Effects onSlightly hazardous in case of skin contact (irritant), of ingestion, of inhalation. Humans Special Remarks onNot available. Toxicity to Animals Special Remarks onMay cause adverse reproductive effects and birth defects (teratogenic) based on animal test data. Chronic Effects on Humans Special Remarks on otherAcute Potential Health Effects: Toxic Effects on HumansSkin: May cause skin irritation. Eyes: May cause eye irritation. Inhalation: May cause respiratory tract irritation. Ingestion: May cause nausea and vomiting. May affect respiration, cardiovascular system. Chronic Potential Health Effects: Ingestion: Prolonged or repeated ingestion may cause weight loss, nausea, vomiting. It may also affect the blood (anemia), adrenal gland. Section 12. Ecological Information EcotoxicityNot available. BOD5 and CODNot available. Possibly hazardous short term degradation products are not likely. However, long term degradation products may Products of Biodegradation arise. The product itself and its products of degradation are not toxic. Toxicity of the Products of Biodegradation Special Remarks on theNot available. Products of Biodegradation Hydrocortisone Sodium Succinate Section 13. Disposal Considerations Waste DisposalWaste must be disposed of in accordance with federal, state and local environmental control regulations. Section 14. Transport Information DOT ClassificationNot a DOT controlled material (United States). Not applicable. Identification Not applicable. Special Provisions for Transport DOT (Pictograms) Section 15. Other Regulatory Information and Pictograms No products were found. Federal and State Regulations CaliforniaCalifornia prop. 65: This product contains the following ingredients for which the State of California has found to cause cancer which would require a warning under the statute: No products were found. Proposition 65 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 RegulationsEINECS: This product is on the European Inventory of Existing Commercial Chemical Substances (EINECS No. 204-725-5). Canada: Listed on Canadian Domestic Substance List (DSL). China: Not listed on National Inventory. Japan: Listed on National Inventory (ENCS). Korea: Listed on National Inventory (KECI). Philippines: Not listed on National Inventory (PICCS). Australia: Listed on AICS. WHMIS (Canada) Not controlled under WHMIS (Canada). Other Classifications DSCL (EEC)This product is not classified according Not applicable. to the EU regulations. 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) Hydrocortisone Sodium Succinate TDG (Canada) (Pictograms) ADR (Europe) (Pictograms) Protective Equipment Gloves. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. SECTION 16 - ADDITIONAL INFORMATION N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : GM9015000 CHEMICAL NAME : Cortisol, succinate, sodium salt CAS REGISTRY NUMBER : 125-04-2 LAST UPDATED : 199612 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C25-H33-O8.Na MOLECULAR WEIGHT : 484.57 WISWESSER LINE NOTATION : L E5 B666 OV MUTJ A1 CQ E1 FVYQOV2VO FQ &-NA- &43/36 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human - man DOSE/DURATION : 2857 ug/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - bronchiolar constriction Gastrointestinal - nausea or vomiting Blood - oxidant related (GPD deficient) anemia REFERENCE : MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 154,210,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1320 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,625,1982 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1050 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,625,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1400 mg/kg/14D-I TOXIC EFFECTS : Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 5,303,1980 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported DOSE : 1429 ug/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - other effects on male Endocrine - androgenic REFERENCE : JCEMAZ Journal of Clinical Endocrinology and Metabolism. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.12- 1952- Volume(issue)/page/year: 57,671,1983 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 1800 mg/kg SEX/DURATION : female 9-14 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - urogenital system REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 4,2969,1970 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 1500 mg/kg SEX/DURATION : female 9-14 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 4,2969,1970 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1600 mg/kg SEX/DURATION : female 6-15 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) REFERENCE : TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 33,68C,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 1200 mg/kg SEX/DURATION : female 7-12 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - physical REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 4,2957,1970 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Ocular DOSE : 120 mg/kg SEX/DURATION : female 10-13 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) REFERENCE : TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 16,175,1977 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 30 mg/kg SEX/DURATION : female 28-30 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - immune and reticuloendothelial system REFERENCE : KRMJAC Kurume Medical Journal. (Kurume Univ. School of Medicine, Dept. of Physiology, 67, Asahi- machi, Kurume 830, Japan) V.1- 1954- Volume(issue)/page/year: 27,51,1980 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular DOSE : 30 mg/kg SEX/DURATION : female 26-28 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - respiratory system REFERENCE : PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 48,547,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3657 No. of Facilities: 589 (estimated) No. of Industries: 3 No. of Occupations: 11 No. of Employees: 13629 (estimated) No. of Female Employees: 8741 (estimated)

安全

• 个人防护装备: Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
• 危害码 (欧洲): Xi
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 3
• RTECS号: GM9015000