胱胺二盐酸盐

胱胺二盐酸盐用途

半胱胺(二盐酸盐)是游离硫醇半胱胺的二硫化物形式。胱胺是一种口服活性转谷氨酰胺酶(Tgase)抑制剂。胱氨酸对caspase-3也具有抑制活性,IC50值为23.6μM。胱胺可用于多种疾病的研究,包括亨廷顿舞蹈症(HD)[1][2][3]。

胱胺二盐酸盐名称

[ CAS 号 ]:
56-17-7

[ 中文名 ]:
胱胺二盐酸盐

[ 英文名 ]:
Cystamine dihydrochloride

[中文别名 ]:

[英文别名 ]:

Ethanamine, 2,2'-dithiobis-, hydrochloride (1:2)
CYSTAMINIUM DICHLORIDE
aed
cystaminedihcl
OYSTAMINE DIHYDROCHLORIDE
2,2'-dithiodiethanamine dihydrochloride
2,2'-diaminodiethyl disulfide dihydrochloride
CystamineHcl
2,2'-Disulfanediyldiethanamine dihydrochloride
2,2'-dithiodiethylamine dihydrocloride

胱胺二盐酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 细胞凋亡 >> 胱天蛋白酶

研究领域 >> 神经疾病

[ 靶点 ]

Caspase 3:23.6 μM (IC50)

[体外研究]

胱胺(二盐酸盐)对caspase-3具有抑制活性,IC50值为23.6μM[1]。胱胺(0-500μM；0-16小时)以浓度依赖的方式抑制重组活性caspase-3[1]。胱胺(250μM；10小时)显著增加谷胱甘肽水平[1]。Western Blot分析[1]细胞系：人神经母细胞瘤SH-SY5Y细胞浓度：250500μM培养时间：0-16小时结果：抑制MG132介导的caspase-3激活。抑制H2O2介导的胱天蛋白酶3激活。以tTG非依赖性方式抑制胱天蛋白酶-3活性。

[体内研究]

胱胺(二盐酸盐)(口服,i.p.；112225 mg/kg)可降低Tgase活性和GGEL水平,降低行为和神经病理学严重程度,并延长R6/2转基因HD小鼠的生存期[2]。动物模型：R6/2转基因HD小鼠[2]剂量：112225 mg/kg给药：腹膜内或口服,每日结果：显著延长生存期,改善体重和运动性能,延缓神经病理后遗症,显著改变Tgase活性和N(Sigma)-(γ-L-谷戊基)-L-赖氨酸(GGEL)水平。

胱胺二盐酸盐物理化学性质

[ 密度 ]:
1.172g/cm3

[ 沸点 ]:
264.8ºC at 760mmHg

[ 熔点 ]:
217-220 °C (dec.)(lit.)

[ 分子式 ]:
C₄H₁₄Cl₂N₂S₂

[ 分子量 ]:
225.203

[ 精确质量 ]:
223.997543

[ PSA ]:
102.64000

[ LogP ]:
3.28980

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 储存条件 ]:
室温

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
soluble

胱胺二盐酸盐MSDS

详细MSDS(安全技术说明书)

胱胺二盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KR7260000

CHEMICAL NAME :: Ethylamine, 2,2'-dithiobis-, dihydrochloride

CAS REGISTRY NUMBER :: 56-17-7

LAST UPDATED :: 199701

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C4-H12-N2-S2.2Cl-H

MOLECULAR WEIGHT :: 225.22

WISWESSER LINE NOTATION :: Z2SS2Z

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 896 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: TOVEFN Toksikologicheskii Vestnik. (18-20 Vadkovskii per. Moscow, 101479, Russia) History Unknown Volume(issue)/page/year: (3),46,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 185,461,1937

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 874 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: TOVEFN Toksikologicheskii Vestnik. (18-20 Vadkovskii per. Moscow, 101479, Russia) History Unknown Volume(issue)/page/year: (3),46,1994

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 405 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 21,284,1971

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 185,461,1937

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 300 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 185,461,1937 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1250 mg/kg

SEX/DURATION :: female 13-17 day(s) after conception

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

REFERENCE :: JEEMAF Journal of Embryology and Experimental Morphology. (Essex, UK) V.1-98, 1953-86. For Publisher information, see DEVPED Volume(issue)/page/year: 8,94,1960 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5832 No. of Facilities: 7 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 1822 (estimated) No. of Female Employees: 272 (estimated)

胱胺二盐酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S37/39-S26-S36/37/39

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

[ WGK德国 ]:
3

[ RTECS号 ]:
KR7260000

[ 海关编码 ]:
29309070

胱胺二盐酸盐上下游产品

胱胺二盐酸盐上游产品

胱胺二盐酸盐下游产品

胱胺二盐酸盐海关

[ 海关编码 ]: 29309070

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