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2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸用途

双氯芬酸，非类固醇抗炎化合物和环氧合酶（COX）抑制剂的代谢物

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2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸名称

[ CAS 号 ]:
64118-84-9

[ 中文名 ]:
4’-羟基双氯芬酸

[ 英文名 ]:
4'-Hydroxy diclofenac

[中文别名 ]:

[英文别名 ]:

4’-Hydroxy Diclofenac
4'-hydroxydiclofenac
4'-Hydroxy Diclofenac

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸生物活性

[ 描述 ]:

4'-Hydroxy diclofenac 是具有口服活性的 Diclofenac (HY-15036) 通过细胞色素 P450 2C9 (CYP2C9) 的代谢产物。4'-Hydroxy diclofenac 具有抗炎和镇痛作用。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

[体内研究]

人源化小鼠单次口服双氯芬酸后,血浆中未发生变化的药物在0.25小时达到峰值,随后下降,半衰期(t1/2)为2.4小时。4’-羟基双氯芬酸也在0.25小时达到峰值,24小时内无法检测。在接受4'-羟基双氯芬酸(10 mg/kg；单次口服)的人源化嵌合小鼠中,4'-羟基双氯芬酸的血浆浓度在0.25小时达到峰值,并迅速下降[2]。

[参考文献]

[1]. J Shimamoto, et al. Lack of Differences in Diclofenac (A Substrate for CYP2C9) Pharmacokinetics in Healthy Volunteers With Respect to the Single CYP2C9*3 Allele. Eur J Clin Pharmacol. 2000 Apr;56(1):65-8.

[2]. Hidetaka Kamimura, et al. Formation of the Accumulative Human Metabolite and Human-Specific Glutathione Conjugate of Diclofenac in TK-NOG Chimeric Mice With Humanized Livers. Drug Metab Dispos. 2015 Mar;43(3):309-16.

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
432.7±45.0 °C at 760 mmHg

[ 熔点 ]:
178-185ºC dec.

[ 分子式 ]:
C₁₄H₁₁Cl₂NO₃

[ 分子量 ]:
312.148

[ 闪点 ]:
215.5±28.7 °C

[ 精确质量 ]:
311.011597

[ PSA ]:
69.56000

[ LogP ]:
4.56

[ 外观性状 ]:
淡紫罗兰色固体

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.690

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
Soluble in DMSO, ethanol or methanol

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸MSDS

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AG6542800

CHEMICAL NAME :: Acetic acid, (o-(2,6-dichloro-4-hydroxyanilino)phenyl)-

CAS REGISTRY NUMBER :: 64118-84-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C14-H11-Cl2-N-O3

MOLECULAR WEIGHT :: 312.16

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 :: 190 mg/kg

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

REFERENCE :: SJRHAT Scandinavian Journal of Rheumatology. (Almqvist & Wiksell, POB 45150, S-10430 Stockholm, Sweden) V.1- 1972- Volume(issue)/page/year: (Suppl 22),5,1978

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2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸安全信息

[ 符号 ]:

GHS02, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H302 + H312 + H332-H319

[ 警示性声明 ]:
P210-P261-P302 + P352 + P312-P304 + P340 + P312-P337 + P313-P403 + P235

[ 个人防护装备 ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T: Toxic;N: Dangerous for the environment;

[ 风险声明 (欧洲) ]:
R25;R37/38;R41;R50/53

[ 安全声明 (欧洲) ]:
S26-S39-S45-S60-S61

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
AG6542800

[ 海关编码 ]:
2922509090

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸合成路线

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸上下游产品

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸上游产品

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸下游产品

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸海关

[ 海关编码 ]: 2922509090

[ 中文概述 ]:
2922509090. 其他氨基醇酚、氨基酸酚及其他含氧基氨基化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件：AB. 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, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: R.进口食品卫生监督检验 S.出口食品卫生监督检验

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

2-((2,6-二氯-4-羟基苯基)氨基)苯乙酸文献

High warfarin sensitivity in carriers of CYP2C9*35 is determined by the impaired interaction with P450 oxidoreductase.

Pharmacogenomics J. 14(4) , 343-9, (2014)

Cytochrome P450 2C9 (CYP2C9) metabolizes many clinically important drugs including warfarin and diclofenac. We have recently reported a new allelic variant, CYP2C9*35, found in a warfarin hypersensiti...

Inhibition of human cytochrome P450 enzymes by licochalcone A, a naturally occurring constituent of licorice.

Toxicol. In Vitro 29 , 1569-76, (2015)

Licochalcone A (LCA) is a major bioactive compound in traditional Chinese herbal liquorice that possesses multiple pharmacological activities. However, the effects of the potential herb-drug interacti...

Structural basis for the 4'-hydroxylation of diclofenac by a microbial cytochrome P450 monooxygenase.

Appl. Microbiol. Biotechnol. 99(7) , 3081-91, (2015)

Diclofenac is a nonsteroidal anti-inflammatory drug. It undergoes hydroxylation by mammalian cytochrome P450 enzymes at 4'- and/or 5'-positions. A bacterial P450 enzyme, CYP105D7 from Streptomyces ave...

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