环孢菌素

环孢菌素 基本信息
CAS号 79217-60-0 分子式 C62H111N11O12
分子量 1202.61000 精确质量 　1201.84000
PSA 　292.76000 LogP 　3.93790
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目录
基本信息 制备方法与用途 物化性质 安全信息 毒性

基本信息 展开↓

CAS号：
79217-60-0
分子式：
C62H111N11O12
分子量：
1202.61000
中文名称：
环孢菌素
英文名称：
Cyclosporine
中文别名：
环孢菌素;
赛斯平;
环孢霉素A
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
精确分子量/精确质量：
1201.84000
极性分子表面积/PSA：
292.76000
油水分配系数/LogP：

LogP值指的是某物质在正辛醇/水两相体系中的分配系数的对数值，反映了物质在油水两相中的分配情况。其中、LogP值越大，说明该物质越亲油；反之，LogP值越小，则说明该物质越亲水。

生产制备方法及用途展开↓

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

物化性质展开↓

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

安全信息展开↓

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

毒理性展开↓

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
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