79217-60-0

• 常用中文名：环孢菌素
• 常用英文名：Cyclosporine
• CAS号：79217-60-0
• 分子式：C₆₂H₁₁₁N₁₁O₁₂
• 分子量：1202.611
• 相关类别： 原料药 抗生素类药物 其它抗生素类药
• 发布时间：2018-02-07 08:00:00
• 更新时间：2024-01-03 13:06:13
• 环孢菌素是一种环状十肽,可从土壤真菌充气菌Tolypocladium inflatum中分离出来。环孢霉素是一种免疫抑制剂,被认为与T淋巴细胞中的亲环蛋白结合[1]。

名称

• 中文名: 环孢菌素
• 英文名: Cyclosporine
• 中文别名: 赛斯平; 环孢霉素A
• 英文别名: cyclosporine; 30-Ethyl-33-[(4E)-1-hydroxy-2-methyl-4-hexen-1-yl]-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone; Cyclosporin; 30-Ethyl-33-[(4E)-1-hydroxy-2-methylhex-4-en-1-yl]-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone; Sandimmune; S1514_Selleck; 30-Ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methyl-4-hexen-1-yl]-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone; Gengraf; 30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone; Neoral; 1,4,7,10,13,16,19,22,25,28,31-Undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone, 30-ethyl-33-[(4E)-1-hydroxy-2-methyl-4-hexen-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-3,21-bis(1-methylethyl)-6,9,18,24-tetrakis(2-methylpropyl)-; 1,4,7,10,13,16,19,22,25,28,31-Undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone, 30-ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methyl-4-hexen-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-3,21-bis(1-methylethyl)-6,9,18,24-tetrakis(2-methylpropyl)-; 30-ethyl-33-[(4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone; MFCD01771104

物化性质

• 密度: 1.0±0.1 g/cm3
• 沸点: 1293.8±65.0 °C at 760 mmHg
• 熔点: 148-151ºC
• 分子式: C₆₂H₁₁₁N₁₁O₁₂
• 分子量: 1202.611
• 闪点: 736.3±34.3 °C
• 精确质量: 1201.841309
• PSA: 292.76000
• LogP: 3.35
• 外观性状: 白色结晶性粉末
• 蒸汽压: 0.0±0.6 mmHg at 25°C
• 折射率: 1.468
• 储存条件: -20°C

生物活性

• 描述: 环孢菌素是一种环状十肽,可从土壤真菌充气菌Tolypocladium inflatum中分离出来。环孢霉素是一种免疫抑制剂,被认为与T淋巴细胞中的亲环蛋白结合[1]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 炎症/免疫
• 体外研究: 环孢菌素(0-2500 nM；Ppia-/-细胞) 以相似的程度抑制 Ppia+/+或 < i> Ppia+/-脾细胞增值,国际50值为 25 nM,Ppia-/-脾细胞的 国际50值至少高出 10倍[1]。 环孢菌素 (0-750 nM；Ppia-/-细胞) 抑制 Ppia-/-细胞中的基因表达[1]。
• 参考文献:

  [1]. Colgan J, et, al. Cyclophilin A-deficient mice are resistant to immunosuppression by cyclosporine. J Immunol. 2005 May 15;174(10):6030-8.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : GZ4110000 CHEMICAL NAME : Cyclosporin CAS REGISTRY NUMBER : 79217-60-0 LAST UPDATED : 199510 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Human - man DOSE/DURATION : 13 mg/kg/13W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes Blood - change in clotting factors REFERENCE : LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 2,1337,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 145 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ANKHEW Antibiotiki i Khimioterapiya. Antibiotics and Chemotherapy. (V/O Me zhdunarodnaya Kniga, 113095 Moskow, USSR) V.33- 1988- Volume(issue)/page/year: 36(10),33,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 280 mg/kg/2W-I TOXIC EFFECTS : Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - body temperature decrease Related to Chronic Data - death REFERENCE : TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 77,181,1985 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 147 mg/kg/21D-I TOXIC EFFECTS : Endocrine - other changes Endocrine - changes in spleen weight Endocrine - changes in thymus weight REFERENCE : ANKHEW Antibiotiki i Khimioterapiya. Antibiotics and Chemotherapy. (V/O Me zhdunarodnaya Kniga, 113095 Moskow, USSR) V.33- 1988- Volume(issue)/page/year: 36(10),33,1991 *** REVIEWS *** IARC Cancer Review:Human Sufficient Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 50,77,1990 IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 50,77,1990 IARC Cancer Review:Group 1 IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 50,77,1990

安全

• 危害码 (欧洲): T, Xn
• 风险声明 (欧洲): 45-60-22-40
• 安全声明 (欧洲): 53-45-36/37-24/25-22