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环孢菌素

环孢菌素用途

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]。

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环孢菌素名称

[ CAS 号 ]:
79217-60-0

[ 中文名 ]:
环孢菌素

[ 英文名 ]:
Cyclosporine

[中文别名 ]:

[英文别名 ]:

cyclosporine
Cyclosporin
Sandimmune
S1514_Selleck
Gengraf
Neoral
MFCD01771104

环孢菌素生物活性

[ 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.

环孢菌素物理化学性质

[ 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

环孢菌素毒性和生态

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

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环孢菌素安全信息

[ 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