促进剂TETD_MSDS_用途_密度_CAS号【97-77-8】

Disulfiram 是特异性的乙醛脱氢酶1型抗体 (ALDH1) 抑制剂,可以通过对酒精产生急性敏感性来治疗慢性酗酒。

点击显示

[ 描述 ]:

Disulfiram 是特异性的乙醛脱氢酶1型抗体 (ALDH1) 抑制剂,可以通过对酒精产生急性敏感性来治疗慢性酗酒。

[ 相关类别 ]:

研究领域 >> 代谢疾病

[体外研究]

在诱导凋亡的癌细胞死亡之前,双硫仑铜复合物有效抑制培养的乳腺癌MDA-MB-231和MCF10DCIS.com细胞中的蛋白酶体活性,但不是正常的永生化MCF-10A细胞[1]。双硫仑(DS)是临床上使用的抗酗酒药物,以剂量依赖性方式强烈抑制组成型和5-FU诱导的NF-κB活性。双硫仑抑制NF-κB核转位和DNA结合活性,但对5-FU诱导的IkappaBalpha降解没有影响。双硫仑显着增强5-FU对DLD-1和RKO(WT)细胞系的细胞凋亡作用,并协同增强5-FU对两种细胞系的细胞毒性。双硫仑还有效地在体外消除5-FU抗性细胞系H630(5-FU)中的5-FU化学抗性[2]。奥塞米韦减少活细胞数量,并且添加CuCl2显着增强DSF诱导的细胞死亡至不到对照的10％[3]。给予黑色素瘤细胞与Cu2 +或Zn2 +联合使用的双硫仑可降低细胞周期蛋白A的表达,并在体外降低浓度,而不是单独使用双硫仑[4]。

[体内研究]

双硫仑显着抑制肿瘤生长(74％),与体内蛋白酶体抑制相关(通过降低肿瘤组织蛋白酶体活性水平和泛素化蛋白和天然蛋白酶体底物p27和Bax的积累来测量)和细胞凋亡诱导(如caspase所示)在携带MDA-MB-231肿瘤异种移植物的小鼠中激活和凋亡细胞核形成[1]。双硫仑阻断P-糖蛋白挤压泵,抑制转录因子核因子-κB,使肿瘤对化学疗法敏感,减少血管生成,并抑制小鼠中的肿瘤生长。双硫仑抑制严重联合免疫缺陷小鼠移植的黑色素瘤的生长和血管生成,这些作用通过补充Zn2 +而得到加强[4]。

[细胞实验]

在用10％FBS刺激的培养物中研究了双硫仑（0.15-5.0μM）或二乙基二硫代氨基甲酸钠（1.0μM）对恶性细胞系增殖的影响。如下所述，细胞数量在24至72小时后定量。在一些实验中，在细胞铺板后立即加入双硫仑。在其他实验中，将细胞铺板并使其生长24至72小时，然后加入含有双硫仑的新鲜培养基并在24至72小时后测定细胞数。在双硫仑与N，N'-双（2-氯乙基-N-亚硝基脲（卡莫司汀，1.0-1,000μM）或顺铂（0.1-100μg/ mL）加入培养基之间研究协同作用。金属离子对双硫仑的影响是用0.2到10μM的Cu2 +（以CuSO4形式提供），Zn2 +（以ZnCl2计），Ag +（如乳酸银）或Au3 +（如HAuCl4·3H2O）离子加入生长培养基中，缓冲至生理pH值。提供生物学相关性铜源，培养基补充人血浆铜蓝蛋白，剂量复制低和高正常成人血清浓度（250和500 mg / mL）。

[动物实验]

将成年雌性CB17-SCID小鼠圈养在受保护的层流设施中，其具有水和含有87ppm锌的标准饮食或含有1,000ppm Zn 2+的锌补充饮食作为乙酸锌。将小鼠皮下注射到来自Carolinas Medical Center患者的高度侵袭性恶性黑素瘤的5×106细胞的右腹股沟。在用于这些实验之前，将冷冻的肿瘤在SCID小鼠中传代两次以使其适应体内生长。在肿瘤注射当天，所有小鼠开始每日施用药物。通过胃管饲法，通过经口部插入胃中的光滑Teflon尖针，给予总体积为0.2mL的药物。研究了四组：肿瘤对照（n = 10;每天0.2mL橄榄油;锌饮食87ppm）;补锌对照组（n = 10;每日0.2 mL橄榄油;锌饮食为1,000 ppm）;双硫仑（n = 10;在0.2 mL橄榄油中200 mg / kg / d双硫仑;锌饮食87 ppm）;和锌补充饮食+双硫仑（n = 10; 200毫克/千克/天双硫仑在0.2毫升橄榄油中;锌饮食为1,000 ppm）。每天检查小鼠，以二维测量肿瘤，并使用椭圆的公式估计肿瘤体积。当在任何动物中估计的肿瘤体积接近500mm 3时，对所有小鼠实施安乐死。切除肿瘤，称重，在福尔马林中固定，切片，染色或免疫染色因子VIII。幻灯片由盲法观察者编码和检查，观察者将血管识别为红细胞沉积物。对于每个载玻片，在代表肿瘤的四个不同区域中计数血管数。每个视野的平均血管数量是每个活检标本的平均值，并用于评估肿瘤血管分布。

[参考文献]

[1]. Chen D, ert al. Disulfiram, a clinically used anti-alcoholism drug and copper-binding agent, induces apoptotic cell death in breast cancer cultures and?xenografts?via?inhibition?of the proteasome?activity. Cancer Res. 2006 Nov 1;66(21):10425-33.

[2]. Wang W, et al. Disulfiram-mediated inhibition of NF-kappaB activity enhances cytotoxicity of 5-fluorouracil in human colorectal cancer cell lines. Int J Cancer. 2003 Apr 20;104(4):504-11.

[3]. Cen D, et al. Disulfiram facilitates intracellular Cu uptake and induces apoptosis in human melanoma cells. J Med Chem. 2004 Dec 30;47(27):6914-20.

[4]. Brar SS, et al. Disulfiram inhibits activating transcription factor/cyclic AMP-responsive element binding protein and human melanoma growth in a metal-dependent manner in vitro, in mice and in a patient with metastatic disease. Mol Cancer Ther. 2004 Sep;3

[相关活性小分子]

阿尔达-1 | NCT-501 | NCT-505

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
369.0±25.0 °C at 760 mmHg

[ 熔点 ]:
69-71 °C(lit.)

[ 分子式 ]:
C₁₀H₂₀N₂S₄

[ 分子量 ]:
296.539

[ 闪点 ]:
177.0±23.2 °C

[ 精确质量 ]:
296.050934

[ PSA ]:
121.26000

[ LogP ]:
3.88

[ 外观性状 ]:
黄色-白色晶体或灰色粉末

[ 蒸汽压 ]:
0.0±0.8 mmHg at 25°C

[ 折射率 ]:
1.620

[ 储存条件 ]:
Store at +4°C

[ 稳定性 ]:
Stable. Incompatible with strong oxidants.

[ 水溶解性 ]:
0.02 g/100 mL

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JO1225000

CHEMICAL NAME :: Disulfide, bis(diethylthiocarbamoyl)

CAS REGISTRY NUMBER :: 97-77-8

LAST UPDATED :: 199806

DATA ITEMS CITED :: 68

MOLECULAR FORMULA :: C10-H20-N2-S4

MOLECULAR WEIGHT :: 296.56

WISWESSER LINE NOTATION :: 2N2&YUS&S 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 140 mg/kg/2W

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 90 mg/kg/18D-I

TOXIC EFFECTS :: Liver - jaundice, other or unclassified

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 150 mg/kg/6W-I

TOXIC EFFECTS :: Musculoskeletal - joints

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 150 mg/kg/6W-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), diffuse

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 160 mg/kg

TOXIC EFFECTS :: Behavioral - coma Gastrointestinal - ulceration or bleeding from large intestine Liver - hepatitis, fibrous (cirrhosis, post-necrotic scarring)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - hallucinations, distorted perceptions Gastrointestinal - nausea or vomiting

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 500 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 248 mg/kg

TOXIC EFFECTS :: Behavioral - changes in motor activity (specific assay) Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >4 gm/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 :: 1980 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 75 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 - mouse

DOSE/DURATION :: 2600 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3500 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1800 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7 gm/kg/7D-I

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic Gastrointestinal - ulceration or bleeding from stomach Blood - changes in spleen

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6750 mg/kg/6W-I

TOXIC EFFECTS :: Brain and Coverings - other degenerative changes Nutritional and Gross Metabolic - changes in metals, not otherwise specified

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7770 mg/kg/3W-I

TOXIC EFFECTS :: Peripheral Nerve and Sensation - recording from peripheral motor nerve Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6545 mg/kg/13W-I

TOXIC EFFECTS :: Autonomic Nervous System - parasympatholytic Gastrointestinal - contraction (isolated tissue) Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 720 mg/kg/60D-I

TOXIC EFFECTS :: Brain and Coverings - other degenerative changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 44640 mg/kg/2Y-C

TOXIC EFFECTS :: 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 :: Mammal - dog

DOSE/DURATION :: 1750 mg/kg/7D-I

TOXIC EFFECTS :: Autonomic Nervous System - other (direct) parasympathomimetic Liver - hepatitis (hepatocellular necrosis), zonal Blood - changes in spleen

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 280 mg/kg/18D-I

TOXIC EFFECTS :: Spinal Cord - demyelination Autonomic Nervous System - other (direct) parasympathomimetic Liver - hepatitis (hepatocellular necrosis), zonal

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 gm/kg/78W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1000 mg/kg

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Blood - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5 gm/kg

SEX/DURATION :: female 3-12 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 310 mg/kg

SEX/DURATION :: male 31 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 400 mg/kg

SEX/DURATION :: female 4-11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

DOSE :: 800 mg/kg

SEX/DURATION :: male 2 day(s) pre-mating female 2 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 13200 mg/kg

SEX/DURATION :: female 15 day(s) pre-mating female 1-18 day(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 39200 mg/kg

SEX/DURATION :: female 7-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1278 mg/kg

SEX/DURATION :: female 6-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 1278 mg/kg

SEX/DURATION :: female 6-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: Morphological transformation

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Bird - chicken Embryo

REFERENCE :: BBACAQ Biochimica et Biophysica Acta. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1947- Volume(issue)/page/year: 519,65,1978 *** REVIEWS *** ACGIH TLV-Not classifiable as a human carcinogen DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 ACGIH TLV-TWA 2 mg/m3 DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 IARC Cancer Review:Animal Inadequate 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: 12,85,1976 IARC Cancer Review:Human No Adequate Data 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: 12,85,1976 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987 TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,365,1973 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-AUSTRALIA:TWA 2 mg/m3 JAN 1993 OEL-BELGIUM:TWA 2 mg/m3 JAN 1993 OEL-FINLAND:TWA 2 mg/m3;STEL 6 mg/m3 JAN 1993 OEL-FRANCE:TWA 2 mg/m3 JAN 1993 OEL-GERMANY:TWA 2 mg/m3 JAN 1993 OEL-THE NETHERLANDS:TWA 2 mg/m3 JAN 1993 OEL-RUSSIA:STEL 1 mg/m3 JAN 1993 OEL-SWITZERLAND:TWA 2 mg/m3 JAN 1993 OEL IN BULGARIA, COLOMBIA, JORDAN, KOREA check ACGIH TLV OEL IN NEW ZEALAND, SINGAPORE, VIETNAM check ACGIH TLV *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH RECOMMENDED EXPOSURE LEVEL (REL) : NIOSH REL TO DISULFIRAM-air:10H TWA 2 mg/m3 REFERENCE : NIOSH* National Institute for Occupational Safety and Health, U.S. Dept. of Health, Education, and Welfare, Reports and Memoranda. Volume(issue)/page/year: DHHS #92-100,1992 NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80219 No. of Facilities: 209 (estimated) No. of Industries: 4 No. of Occupations: 24 No. of Employees: 4441 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80219 No. of Facilities: 2688 (estimated) No. of Industries: 28 No. of Occupations: 51 No. of Employees: 53525 (estimated) No. of Female Employees: 6305 (estimated)

点击显示

[ 符号 ]:

GHS07, GHS08, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H317-H373-H410

[ 警示性声明 ]:
P273-P280-P501

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22;R43;R48/22;R50/53

[ 安全声明 (欧洲) ]:
S24-S37-S60-S61

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
JO1225000

[ 包装等级 ]:
III

[ 危险类别 ]:
9

[ 海关编码 ]:
29303000

详细合成路线

促进剂TETD上游产品

促进剂TETD下游产品

1、二乙基二硫代氨基甲酸钠的制备在密度为1.075kg/m3（10°Bé）的碱液中，搅拌下加入二乙胺、二硫化碳，加热至40～45℃，缩合反应2h，当pH值为常数时，即为反应终点。反应生成二乙基二硫代氨基甲酸钠。

2、促进剂TETD的制备将10%的亚硝酸钠水溶液，在常温下滴加入上步反应的生成物中，搅拌混合均匀，物料成草绿色。经过滤去渣，再滴加入4%的稀硫酸，并鼓入空气，控制反应温度低于10℃。反应生成的促进剂TETD以固体粒子析出。待反应完全，出料过滤，滤饼经水洗、离心脱水、干燥、筛选，即为成品。

点击显示

[ 海关编码 ]: 29303000

An orphan esterase ABHD10 modulates probenecid acyl glucuronidation in human liver.

Drug Metab. Dispos. 42(12) , 2109-16, (2014)

Probenecid, a widely used uricosuric agent, is mainly metabolized to probenecid acyl glucuronide (PRAG), which is considered a causal substance of severe allergic or anaphylactoid reactions. PRAG can ...

Magnetic high throughput screening system for the development of nano-sized molecularly imprinted polymers for controlled delivery of curcumin.

Analyst 140(9) , 3113-20, (2015)

Curcumin is a versatile anti-inflammatory and anti-cancer agent known for its low bioavailability, which could be improved by developing materials capable of binding and releasing drug in a controlled...

Metabolic characterization of meso-dihydroguaiaretic acid in liver microsomes and in mice.

Food Chem. Toxicol. 76 , 94-102, (2015)

meso-Dihydroguaiaretic acid (MDGA) is a major component of Myristica fragrans and Machilus thunbergii that is traditionally used as a spice and for medicinal purposes. Despite reports of various biolo...

更多文献