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柳氮磺胺吡啶

柳氮磺胺吡啶用途

Sulfasalazine是治疗类风湿关节炎和溃疡性结肠炎的药物。报道显示Sulfasalazine可抑制 NF-κB 的活性。

柳氮磺胺吡啶名称

[ CAS 号 ]:
599-79-1

[ 中文名 ]:
柳氮磺吡啶

[ 英文名 ]:
sulfasalazine

[中文别名 ]:

[英文别名 ]:

salazosulfapyridine
reupirin
sulcolon
salisulf
EINECS 209-974-3
Salicylazosulfapyridine
azopyrin
sas-500
si-88
MFCD00057363

柳氮磺胺吡啶生物活性

[ 描述 ]:

Sulfasalazine是治疗类风湿关节炎和溃疡性结肠炎的药物。报道显示Sulfasalazine可抑制 NF-κB 的活性。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> NF-κB信号通路 >> NF-κB

研究领域 >> 炎症/免疫

[ 靶点 ]

RelA

Autophagy

[体外研究]

用柳氮磺胺吡啶处理SW620结肠细胞抑制TNFα-,LPS-或佛波醇酯诱导的NFκB活化。在微量至毫摩尔浓度下,柳氮磺胺吡啶可抑制NFκB依赖性转录。通过抑制IκBα降解,柳氮磺胺吡啶可以预防TNFα诱导的NFκB核转位[1]。与载体对照相比,单独用5mM柳氮磺吡啶预孵育显着增加所有促炎细胞因子的基础mRNA表达,IL-6 mRNA水平增加80倍[2]。一旦被消化,柳氮磺胺吡啶被结肠细菌切割成磺胺吡啶和5-氨基水杨酸,后者也被报道抑制NF-κB活性[3]。

[体内研究]

在低剂量(0.25 mM)下,与未经治疗的对照相比,SAS能够抑制胶质瘤生长超过60％[3]。

[细胞实验]

柳氮磺胺吡啶溶解在培养基中。 SW620细胞在Dulbecco改良的Eagle培养基中生长，补充有10％热灭活的FCS，2mmol /升谷氨酰胺和1％（wt / vol）青霉素/链霉素。用3xIgkBLuc报道构建体转染SW620细胞。 18小时后，在用TNFα，LPS或PMA刺激之前，将细胞与单独的培养基或柳氮磺胺吡啶（0.1,0.2,0.5,1,2,5mM）一起温育。进行荧光素酶测定[1]。

[动物实验]

小鼠：将柳氮磺胺吡啶溶于0.1M NaOH中，然后用0.1M HCl滴定中和。将U-87MG神经胶质瘤细胞植入SCID小鼠的颅骨中。 7天后，将动物随机分成三组，每组五只动物。一组每天两次接受1mL ip盐水注射，持续3周。两个试验组每天两次在1mL盐水中接受8mg柳氮磺吡啶，持续3周。监测肿瘤生长和动物健康。用4％多聚甲醛灌注后，收集小鼠脑，冲洗，并置于30％蔗糖中[3]。

[参考文献]

[1]. Wahl C, et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. J Clin Invest. 1998 Mar 1;101(5):1163-74.

[2]. Sykes L, et al. Sulfasalazine augments a pro-inflammatory response in interleukin-1β-stimulated amniocytes and myocytes. Immunology. 2015 Dec;146(4):630-44.

[3]. Chung WJ, et al. Sulfasalazine inhibits the growth of primary brain tumors independent of nuclear factor-kappaB. J Neurochem. 2009 Jul;110(1):182-93.

[相关活性小分子]

柳氮磺胺吡啶物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
689.3±65.0 °C at 760 mmHg

[ 熔点 ]:
260-265 °C (dec.)(lit.)

[ 分子式 ]:
C₁₈H₁₄N₄O₅S

[ 分子量 ]:
398.393

[ 闪点 ]:
370.7±34.3 °C

[ 精确质量 ]:
398.068481

[ PSA ]:
149.69000

[ LogP ]:
3.18

[ 外观性状 ]:
黄色至棕色粉末

[ 蒸汽压 ]:
0.0±2.3 mmHg at 25°C

[ 折射率 ]:
1.691

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
NH4OH 1 M: 50 mg/mL, clear, red | <0.1 g/100 mL at 25 ºC

柳氮磺胺吡啶MSDS

详细MSDS(安全技术说明书)

柳氮磺胺吡啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VO6250000

CHEMICAL NAME :: Salicylic acid, 5-((p-(2-pyridylsulfamoyl)phenyl)azo)-

CAS REGISTRY NUMBER :: 599-79-1

BEILSTEIN REFERENCE NO. :: 0356241

LAST UPDATED :: 199803

DATA ITEMS CITED :: 38

MOLECULAR FORMULA :: C18-H14-N4-O5-S

MOLECULAR WEIGHT :: 398.42

WISWESSER LINE NOTATION :: T6NJ BSWMR DNUNR DQ CVQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1286 mg/kg/30D-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes Blood - eosinophilia Blood - changes in cell count (unspecified)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 570 mg/kg/11D-I

TOXIC EFFECTS :: Blood - leukopenia Blood - thrombocytopenia Blood - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 3800 mg/kg/19D-I

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7143 ug/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 143 mg/kg/10D-I

TOXIC EFFECTS :: Blood - thrombocytopenia

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 3200 mg/kg/31D-I

TOXIC EFFECTS :: Blood - agranulocytosis Blood - other changes Skin and Appendages - dermatitis, allergic (after systemic exposure)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human

DOSE/DURATION :: 429 mg/kg/10D-I

TOXIC EFFECTS :: Blood - other hemolysis with or without anemia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 357 mg/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - headache

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

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

TOXIC EFFECTS :: Behavioral - headache Gastrointestinal - hypermotility, diarrhea Nutritional and Gross Metabolic - body temperature increase

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1300 mg/kg/4W-I

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - ataxia Gastrointestinal - nausea or vomiting

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 2700 mg/kg/13W-I

TOXIC EFFECTS :: Skin and Appendages - dermatitis, other (after systemic exposure) Immunological Including Allergic - uncharacterized

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Rectal

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7143 ug/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 15600 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 :: 3870 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 :: 1520 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 :: 12500 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 :: 3 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1096 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 :: >7500 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 :: 32400 mg/kg/16D-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Endocrine - changes in thymus weight 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 - mouse

DOSE/DURATION :: 32400 mg/kg/16D-I

TOXIC EFFECTS :: Gastrointestinal - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 177 mg/kg/2Y-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Kidney, Ureter, Bladder - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 141 mg/kg/2Y-I

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8100 mg/kg

SEX/DURATION :: female 1-40 week(s) after conception

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5460 mg/kg

SEX/DURATION :: male 13 week(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 :: Oral

DOSE :: 8400 mg/kg

SEX/DURATION :: male 28 day(s) pre-mating

TOXIC EFFECTS :: 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 :: Oral

DOSE :: 16800 mg/kg

SEX/DURATION :: male 28 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7 gm/kg

SEX/DURATION :: male 35 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 :: Oral

DOSE :: 8400 mg/kg

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

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

DOSE :: 43875 mg/kg

SEX/DURATION :: male 13 week(s) pre-mating

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

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 5634 mg/kg

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 283,53,1992 *** REVIEWS *** TOXICOLOGY REVIEW DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 1(8),8,1981 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5355 No. of Facilities: 48 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 704 (estimated) No. of Female Employees: 435 (estimated)

柳氮磺胺吡啶安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H317-H334

[ 警示性声明 ]:
P261-P280-P284-P304 + P340-P333 + P313-P342 + P311

[ 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) ]:
R42/43

[ 安全声明 (欧洲) ]:
S22-S29/56-S45

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

[ WGK德国 ]:
2

[ RTECS号 ]:
VO6250000

[ 海关编码 ]:
2935009090

柳氮磺胺吡啶合成路线

详细合成路线

柳氮磺胺吡啶上下游产品

柳氮磺胺吡啶上游产品

柳氮磺胺吡啶下游产品

柳氮磺胺吡啶制备

二、制备方法：2-氨基吡啶与N-乙酰氨基-苯磺酰氯反应，随后水解得到磺酰吡啶胺，即磺胺吡啶，磺胺吡啶重氮化后与水杨酸偶合、酸化即制得柳氮磺胺吡啶。

柳氮磺胺吡啶海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

柳氮磺胺吡啶文献

Diplacone and mimulone ameliorate dextran sulfate sodium-induced colitis in rats.

Fitoterapia 101 , 201-7, (2015)

Diplacone (1) and mimulone (2), two geranylated flavanones, have previously shown anti-inflammatory and antiradical activity in vitro. The present study aimed to evaluate their activity in vivo on a m...

Sulfa drugs inhibit sepiapterin reduction and chemical redox cycling by sepiapterin reductase.

J. Pharmacol. Exp. Ther. 352(3) , 529-40, (2015)

Sepiapterin reductase (SPR) catalyzes the reduction of sepiapterin to dihydrobiopterin (BH2), the precursor for tetrahydrobiopterin (BH4), a cofactor critical for nitric oxide biosynthesis and alkylgl...

Targeted adsorption of molecules in the colon with the novel adsorbent-based medicinal product, DAV132: A proof of concept study in healthy subjects.

J. Clin. Pharmacol. 55(1) , 10-6, (2014)

During antibiotic treatments, active residuals reaching the colon profoundly affect the bacterial flora resulting in the emergence of resistance. To prevent these effects, we developed an enteric-coat...

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