环孢霉素A_MSDS_用途_密度_环孢霉素ACAS号【59865-13-3】

Cyclosporin A 是一种免疫抑制剂,能与亲环素结合,抑制 calcineurin 活性的IC50 值为 7 nM。

[ 描述 ]:

Cyclosporin A 是一种免疫抑制剂,能与亲环素结合,抑制 calcineurin 活性的IC50 值为 7 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 7 nM (calcineurin)

[体外研究]

环孢菌素A能够与T细胞中的亲环蛋白结合[1]。环孢菌素A通过形成亲环蛋白-环孢菌素A复合物来抑制神经钙蛋白[2]。环孢菌素A对钙调神经磷酸酶具有抑制作用,IC50为7 nM [3]。环孢菌素A抑制NF-AT的核转位[4]。环孢菌素A通过阻止MTP打开显示对线粒体的影响,IC50为39 nM [5]。

[体内研究]

环孢菌素A具有免疫抑制活性,并且在小鼠,大鼠和豚鼠中通过肠胃外和口服给药具有活性[6]。环孢菌素A可用于器官移植以防止排斥反应[7]。

[激酶实验]

与纯化酶的反应混合物含有100 nM钙调神经磷酸酶，100 nM钙调蛋白和5μM32P标记的磷酸肽，在60μL（总体积）的含有20 mM Tris（pH 8），100 mM NaCl，6 mM MgCl 2,0.5的分析缓冲液中mM二硫苏糖醇，每毫升0.1mg牛血清白蛋白，和0.1mM CaCl 2或5mM EGTA。与细胞裂解物的反应混合物含有20μL未稀释的裂解物，5μM32P标记的磷酸肽和40μL测定缓冲液。反应混合物含有50μM肽412或413和/或500nM冈田酸，磷酸酶1和2A的特异性抑制剂; 500nM冈田酸足以抑制Ca2 +非依赖性磷酸酶，而较高浓度也部分抑制Ca2 +依赖性磷酸酶活性。在30℃下15分钟后，通过加入0.5mL含有5％三氯乙酸的100mM磷酸钾缓冲液（pH7.0）终止反应。通过Dowex阳离子交换色谱法分离游离无机磷酸盐，并如所述通过闪烁计数进行定量。

[细胞实验]

免疫抑制剂以比细胞处理所需浓度高1000倍的浓度溶解在乙醇中。将细胞（106）悬浮于微量离心管中的1mL完全培养基中;加入1μL乙醇或环孢菌素A的乙醇溶液，并将细胞在37℃下孵育1小时。将细胞在冰上用1mL PBS洗涤两次，并在含有50mM Tris（pH 7.5）的50μL低渗缓冲液中裂解; 0.1mM EGTA; 1 mM EDTA; 0.5mM二硫苏糖醇;每毫升50μg苯甲基磺酰氟，50μg大豆胰蛋白酶抑制剂，5μg亮肽素和5μg抑肽酶。将裂解物在液氮中进行三个循环的冷冻，然后在30℃下解冻，然后在4℃下以12,000×g离心10分钟。

[动物实验]

在第0天腹膜内用0 5mL免疫大鼠，小鼠静脉内用0 2mL 10％洗过的绵羊红细胞（SE）悬浮液免疫。为了引起二次反应，在初次免疫后8-11周，用静脉内注射0-2mL的25％洗涤的SE（107个细胞）对小鼠进行加强免疫。对于长期治疗，动物在13周内每天在食物中平均接受45mg / kg环孢菌素A.在杀死前5天对这些大鼠进行免疫。

[参考文献]

[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7.

[2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15.

[3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90.

[4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7.

[5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92.

[6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25.

[7]. Williams, R, et al. Randomised trial comparing tacrolimus (FK506) and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428.

[相关活性小分子]

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
1293.8±65.0 °C at 760 mmHg

[ 熔点 ]:
148-151°C

[ 分子式 ]:
C₆₂H₁₁₁N₁₁O₁₂

[ 分子量 ]:
1202.611

[ 闪点 ]:
736.3±34.3 °C

[ 精确质量 ]:
1201.841309

[ PSA ]:
278.80000

[ LogP ]:
3.35

[ 外观性状 ]:
从-15℃的丙酮得白色针状结晶，熔点148～151℃，[α]D20-244°(C=0.6，氯仿)。溶于甲醇、乙醇、丙酮、乙醚或氯仿，微溶于水及饱和碳氢化合物。急性毒性LD50小鼠，大鼠，兔子(mg/kg)：107，25，＞10静脉注射；2329，1480，＞1000口服。

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.468

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
ethanol: 30 mg/mL

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GZ4120000

CHEMICAL NAME :: Cyclosporin A

CAS REGISTRY NUMBER :: 59865-13-3

LAST UPDATED :: 199801

DATA ITEMS CITED :: 35

MOLECULAR FORMULA :: C62-H111-N11-O12

MOLECULAR WEIGHT :: 1202.84

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 1911 mg/kg/91W-I

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 62500 ug/kg/5D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Nutritional and Gross Metabolic - body temperature increase

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 20 mg/kg/2D-I

TOXIC EFFECTS :: Behavioral - headache Vascular - acute arterial occlusion Lungs, Thorax, or Respiration - cyanosis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 12 mg/kg

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section Endocrine - antidiuresis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 30 mg/kg/4D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1480 mg/kg

TOXIC EFFECTS :: Behavioral - muscle contraction or spasticity Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 147 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 286 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 24 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2329 mg/kg

TOXIC EFFECTS :: Behavioral - muscle contraction or spasticity Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 96 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Behavioral - muscle contraction or spasticity Gastrointestinal - hypermotility, diarrhea Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 140 mg/kg/14D-I

TOXIC EFFECTS :: Endocrine - changes in spleen weight Blood - changes in spleen

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 350 mg/kg/7D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - multiple enzyme effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 800 mg/kg/10D-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 420 mg/kg/28D-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Musculoskeletal - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 700 mg/kg/28D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 210 mg/kg/14D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - renal function tests depressed Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg/40D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Metabolism (Intermediary) - amino acids (including renal excretion) Biochemical - Metabolism (Intermediary) - Plasma proteins not involving coagulation

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 140 mg/kg/7D-I

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section Vascular - regional or general arteriolar or venous dilation

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg/3D-I

TOXIC EFFECTS :: Vascular - BP elevation not characterized in autonomic section Vascular - structural changes in vessels Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 259 mg/kg/2W-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Blood - lymphoma, including Hodgkin's disease

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 166 mg/kg

SEX/DURATION :: male 45 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - other effects on male Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 420 mg/kg

SEX/DURATION :: male 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 560 mg/kg

SEX/DURATION :: male 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - other effects on male

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 90 mg/kg

SEX/DURATION :: female 6-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 50 mg/kg

SEX/DURATION :: female 12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 210 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Fertility - other measures of fertility

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 1 mg/L

REFERENCE :: IGAYAY Igaku No Ayumi. Progress in Medicine. (Ishiyaku Shuppan K.K., 1-7-10, Honkomagom, Bunkyo-ku, Tokyo, Japan) V.1- 1946- Volume(issue)/page/year: 134,403,1985 *** 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

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H350-H360

[ 警示性声明 ]:
P201-P301 + P312 + P330-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic

[ 风险声明 (欧洲) ]:
R45;R60;R22

[ 安全声明 (欧洲) ]:
53-45-36/37-24/25-22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
GZ4120000

[ 海关编码 ]:
2941909000

环孢霉素A上游产品

环孢霉素A下游产品

1.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。

2.以多孢木霉菌为生产菌株。先制备环孢素发酵液。向发酵液中加入乙酸乙酯提取，分出有机层，减压蒸发，得粗品。经纯化处理可得。

[ 海关编码 ]: 2941909000

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公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：环孢菌素A

公司名：云南西力生物技术股份有限公司

区域：昆明市盘龙区

价格：
￥需询单/5mg

联系人：郑雪平

产品详情：环孢菌素A

公司名：上海吉至生化科技有限公司

区域：上海市奉贤区

价格：
￥158.0/250mg ￥458.0/1g ￥158.0/20mg

联系人：刘佳

产品详情：环胞霉素A

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Cyclosporin A

公司名：上海脉铂医药科技有限公司

区域：上海市嘉定区

价格：
￥400.0/100mg ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：李先生

产品详情：环孢菌素

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