环孢菌素

基本信息
制备方法及用途
物化性质
安全信息
毒理性

环孢菌素基本信息

中文名称：: 环孢菌素

中文别名：: 环孢菌素;
赛斯平;
环孢霉素A

英文名称：: Cyclosporine

英文别名：: Cyclosporine;
Neoral;
Cyclosporin;
cyclosporine;
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;
Gengraf;
Sandimmune

CAS No.：: 79217-60-0

分子式：: C62H111N11O12

分子量：: 1202.61

精确分子量：: 1201.84000

PSA：: 292.76000

风险术语：: R45; R60; R22; R40

分子结构式：

SDS：: 查看

环孢菌素制备方法及用途

制备方法

以多孢木霉菌(Tolypocladium inflatum Cams)为生产菌株。75L罐内装50L种子培养基,接种5×109个孢子,Ph=5.4—4.3,培养72h,得到一级种子液。750L发酵罐内装500L发酵培养基,种入上述一级种子液,培养6天,得二级种子液。4500L发酵罐内装3000L发酵培养基,发酵12天,得到环孢素发酵毒。往发酵液中加人等体积的乙酸乙酯提取,分出有机层,减压蒸发,得粗品。融化处理,可得环孢素和环孢菌素C组分,其中环孢素的产量约为150～200mg/L环孢菌素C约为50～100mg/L。

用途简介

用于治疗白血病、癌、肾移植、结核病等

环孢菌素物化性质

外观与性状：: 白色结晶性粉末
密度：: 1.016g/cm3
熔点：: 148-151ºC
沸点：: 1293.8ºC at 760 mmHg
闪点：: 736.3ºC
折射率：: 1.467

环孢菌素安全信息

危险类别码：: 45-60-22-40
安全说明：: 53-45-36/37-24/25-22
危险标志：: T, Xn

环孢菌素毒理性

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