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舒林酸

舒林酸用途

Sulindac 是一种非甾体类抗炎剂,能够抑制 COX-2 的活性,同时可抑制 COX-2 的过表达。

舒林酸名称

[ CAS 号 ]:
38194-50-2

[ 中文名 ]:
舒林酸

[ 英文名 ]:
Sulindac

[中文别名 ]:

硫茚酸

[英文别名 ]:

AFLODAC
Imbaral
Saldac
SULREUMA
MFCD00599589
Sudac
Aclin
ReuMyl
SULINOL
mobilin

舒林酸生物活性

[ 描述 ]:

Sulindac 是一种非甾体类抗炎剂,能够抑制 COX-2 的活性,同时可抑制 COX-2 的过表达。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 免疫及炎症 >> COX

研究领域 >> 炎症/免疫

[ 靶点 ]

COX-2

Autophagy

[体外研究]

舒林酸是一种非甾体类抗炎药,可作为COX-2抑制剂,抑制COX-2的过度表达[1]。舒林酸(0.1 mM至0.5 mM)导致p53 wt和p53 null HCT116细胞死亡有限,但与维生素C组合,相对于单独的维生素C,p53 wt HCT116细胞的细胞死亡率显着增加近5倍,这种作用涉及这些细胞中的半胱天冬酶活化和p53功能,并通过ROS介导的途径。舒林酸联合维生素C可显着提高PUMA水平,但对Bim,Bcl-2和Mcl-1水平没有影响[2]。舒林酸(500μM)与塞来昔布联合阻断转化生长因子(TGF)-β1诱导的A549细胞上皮-间质转化,迁移和侵袭。该组合还抑制sirtuin 1(SIRT1)参与转化生长因子(TGF)-β1诱导的上皮-间质转化(EMT)[3]。

[体内研究]

舒林酸(0.5±0.1毫克/天)可降低COX,改善PGE2水平并防止Min小鼠肿瘤形成[1]。

[细胞实验]

用指定剂量的舒林酸和/或维生素C处理细胞48小时，并使用台盼蓝排除测定法分析细胞活力。对于膜联蛋白V染色测定，用0.5mM舒林酸和/或0.5mM维生素C处理细胞48小时。然后将细胞用胰蛋白酶消化，用PBS洗涤，用碘化丙锭（PI）和FITC标记的膜联蛋白V染色30分钟，并使用荧光激活细胞分选仪通过流式细胞术分析[2]。

[动物实验]

小鼠[1]在5周龄的雌性C57BL16J-Min / +（Min）小鼠用于测定。从5-6周开始，给10只小鼠喂食用0.001％乙氧基喹啉和舒林酸修饰的低脂肪AIN-76A饲料，0.5±0.1mg /天（0.05mg / kcal /天或约160ppm）。饮用水。作为对照，9只小鼠和5只C57BL / 6J - + / +不受影响的同窝仔（+ / +）喂食AIN-76A饮食，不含舒林酸。每天检查动物的窘迫或贫血症状。每周两次称重动物及其食物。在实验过程中，各研究组的体重或食物消耗没有差异。在Min / Sulindac组中没有观察到毒性。在110日龄时，通过吸入CO 2对所有小鼠实施安乐死，并将其肠道从食道移至远端直肠，打开，用盐水冲洗，并在×3放大倍数下检查以获得肿瘤计数。肿瘤由对动物遗传状态和治疗不知情的个体计数。从小肠中段收获多个大致正常的全厚度肠样品，或者在液氮中冷冻或者在10％福尔马林中固定用于组织学检查。本研究中用于分析的所有样本均取自小肠中段[1]。

[参考文献]

[1]. Boolbol SK, et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Res. 1996 Jun 1;56(11):2556-60.

[2]. Gong EY, et al. Combined treatment with vitamin C and sulindac synergistically induces p53- and ROS-dependent apoptosis in human colon cancer cells. Toxicol Lett. 2016 Sep 6;258:126-133.

[3]. Cha BK, et al. Celecoxib and sulindac inhibit TGF-β1-induced epithelial-mesenchymal transition and suppress lung cancer migration and invasion via downregulation of sirtuin 1. Oncotarget. 2016 Aug 30;7(35):57213-57227.

[相关活性小分子]

舒林酸物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
581.6±50.0 °C at 760 mmHg

[ 熔点 ]:
182-185°C

[ 分子式 ]:
C₂₀H₁₇FO₃S

[ 分子量 ]:
356.411

[ 闪点 ]:
305.6±30.1 °C

[ 精确质量 ]:
356.088257

[ PSA ]:
73.58000

[ LogP ]:
3.59

[ 外观性状 ]:
黄色固体

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.673

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
水溶性：不溶；极微溶：醇,甲醇

舒林酸MSDS

详细MSDS(安全技术说明书)

舒林酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NK8226000

CHEMICAL NAME :: 1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-((4-(methylsulfinyl)phenyl)methyl ene)-, (Z)-

CAS REGISTRY NUMBER :: 38194-50-2

LAST UPDATED :: 199612

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C20-H17-F-O3-S

MOLECULAR WEIGHT :: 356.43

WISWESSER LINE NOTATION :: L56 BYJ BU1R DSO&1& C1 D1VQ GF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 43 mg/kg/10D-I

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes Liver - liver function tests impaired Blood - leukopenia

REFERENCE :: JAMAAP JAMA, Journal of the American Medical Association. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1883- Volume(issue)/page/year: 244,269,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 112 mg/kg/2W-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Liver - hepatitis (hepatocellular necrosis), diffuse Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 10,512,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 8 mg/kg/10H-I

TOXIC EFFECTS :: Behavioral - anorexia (human) Behavioral - muscle contraction or spasticity Gastrointestinal - hypermotility, diarrhea

REFERENCE :: JCGADC Journal of Clinical Gastroenterology. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) Volume(issue)/page/year: 8,569,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 34 mg/kg/6D-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - changes in potassium

REFERENCE :: JRHUA9 Journal of Rheumatology. (920 Yonge St., Suite 608, Toronto, Ont., Canada) V.1- 1974- Volume(issue)/page/year: 13,1084,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 264 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: 30,1398,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 289 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 336 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 507 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,APP-6,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 305 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 398 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 13,637,1982 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4 mg/kg

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

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

REFERENCE :: JCGBDF Journal of Craniofacial Genetics and Developmental Biology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 10,83,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 4 mg/kg

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

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

REFERENCE :: JCGBDF Journal of Craniofacial Genetics and Developmental Biology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 10,83,1990 *** REVIEWS *** TOXICOLOGY REVIEW DSMJAA Delaware Medical Journal. (Medical Soc. of Delaware, 1925 Lovering Ave., Wilmington, DE 19806) V.32(2)- 1960- Volume(issue)/page/year: 53,193,1981 TOXICOLOGY REVIEW REPTED Reproductive Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1987- Volume(issue)/page/year: 9,7,1995 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5356 No. of Facilities: 81 (estimated) No. of Industries: 2 No. of Occupations: 9 No. of Employees: 4344 (estimated) No. of Female Employees: 1829 (estimated)

舒林酸安全信息

[ 符号 ]:

GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H317-H334-H361

[ 警示性声明 ]:
Missing Phrase - N15.00950417-P261-P280-P284-P304 + P340-P342 + P311

[ 个人防护装备 ]:
Eyeshields;Faceshields;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) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 危险品运输编码 ]:
3249

[ RTECS号 ]:
NK8226000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2930909090

舒林酸上下游产品

舒林酸上游产品

舒林酸下游产品

舒林酸制备

方法1：4-硝基邻苯二甲酸经氢化还原为4-氨基邻苯二甲酸，经Schiemann反应生成4-氟邻苯二甲酸，酯化为4-氟邻苯二甲酸二乙酯，和丙酸乙酯在钠作用下缩合环合，生成二氢茚，再和有机膦化合物反应，在3位引入乙酸甲酯，接着和对甲亚磺酰基苄基溴进行格氏反应，最后水解得舒林酸

方法4；5-氟-2-甲基-1-氧代-2，3-二氢-1H-茚和对甲硫基苄基氯进行格氏反应，在1位引入对甲硫基苄基，然后在酸性中脱水，在1，2位形成双键，再和乙醛酸反应，在3位引入乙酸基，双氧水氧化，最后酸化使双键移位得到舒林酸。

舒林酸海关

[ 海关编码 ]: 2930909090

[ 中文概述 ]:
2930909090. 其他有机硫化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

舒林酸文献

Pharmacological protection of retinal pigmented epithelial cells by sulindac involves PPAR-α.

Proc. Natl. Acad. Sci. U. S. A. 111(47) , 16754-9, (2014)

The retinal pigmented epithelial (RPE) layer is one of the major ocular tissues affected by oxidative stress and is known to play an important role in the etiology of age-related macular degeneration ...

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

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舒林酸