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萘普生钠

萘普生钠用途

Naproxen sodium 是COX-1 和 COX-2 的抑制剂,在细胞试验中 IC50 值分别为8.72和5.15 μM.

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萘普生钠名称

[ CAS 号 ]:
26159-34-2

[ 中文名 ]:
甲氧奈丙酸钠

[ 英文名 ]:
naproxen sodium

[中文别名 ]:

[英文别名 ]:

EINECS 247-486-2
sodium (S)-2-(6-methoxynaphthalen-2-yl)propanoate
Anaprox,Naprelan
(S)-Naproxen Sodium Salt
Naproxen sodium
MFCD00058507
Naproxen (sodium)

萘普生钠生物活性

[ 描述 ]:

Naproxen sodium 是COX-1 和 COX-2 的抑制剂,在细胞试验中 IC50 值分别为8.72和5.15 μM.

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

研究领域 >> 炎症/免疫

[ 靶点 ]

COX-2:5.65 μM (IC50, in intact cells )

COX-1:9.55 μM (IC50, in intact cells )

[体外研究]

Naproxen etemesil是一种亲脂性,非酸性,无活性的萘普生前药,一旦被吸收就会水解成药理活性的萘普生。萘普生是一种众所周知的非甾体抗炎药。 Naproxen在完整细胞中大约是COX-1和COX-2的等效抑制剂,IC50分别为2.2μg/ mL和1.3μg/ mL [1]。

[体内研究]

萘普生在博来霉素诱导的肺纤维化小鼠模型中发挥抗炎和抗纤维化作用。萘普生还可下调TGF-β水平和Smad3/4复合物的形成[2]。萘普生可以抑制疼痛,发热和PGE2的时间过程,具有相似的效力(IC50 =27,40,13μM)[3]。

[细胞实验]

将BAEC与萘普生（0.1ng / mL至1mg / mL）孵育30分钟。然后加入花生四烯酸（30μM），并将细胞在37℃下再温育15分钟。然后除去培养基，放射免疫测定用于测量6-酮-PGF，a，PGE2，血栓素B2或PGF2a的形成[1]。

[动物实验]

大鼠[3]为了测量骆驼素在单关节炎的卡拉胶诱导模型中的镇痛作用，将雄性Sprague-Dawley大鼠（n = 48,217±28 g）随机分成4组，每组12只，通过内部开发的计算机程序，盲目表现行为实验。为了通过炎症诱导痛觉过敏，1B组，1C组和1D组中的动物在异氟烷麻醉下（时间= -1h）在左后肢接受40μL关节内注射含有7.5mg / mL角叉菜胶的盐水溶液。 1A组动物不接受注射。 1小时后（时间= 0），组1A，1B，1C和1D中的动物分别在0,0,7.5和30μmol/ kg的盐水中接受口服剂量的萘普生。测量的剂量和时间点是根据预测在实验时间跨度内测量完整浓度 - 效应关系的模拟来选择的[3]。将小鼠[2]博来霉素（0.05IU）气管内滴注至C57BL / 6小鼠，然后用载体JNJ7777120（40mg / kg b.wt。），萘普生（21mg / kg b）的微渗透泵处理。 wt。），或两者的组合。评估气道对通气的抵抗力，肺硬度指数，并对肺标本进行炎症，氧化应激和纤维化标志物处理[2]。

[参考文献]

[1]. Mitchell JA, et al. Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc Natl Acad Sci U S A. 1993 Dec 15;90(24):11693-7.

[2]. Rosa AC, et al. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ7777120 treatment. J Pharmacol Exp Ther. 2014 Nov;351(2):308-16.

[3]. Krekels EH, et al. Pharmacokinetic-pharmacodynamic modeling of the inhibitory effects of naproxen on the time-courses of inflammatory pain, fever, and the ex vivo synthesis of TXB2 and PGE2 in rats.

[相关活性小分子]

萘普生钠物理化学性质

[ 沸点 ]:
403.9ºC at 760 mmHg

[ 熔点 ]:
250-251ºC

[ 分子式 ]:
C₁₄H₁₃NaO₃

[ 分子量 ]:
252.241

[ 闪点 ]:
154.5ºC

[ 精确质量 ]:
252.076233

[ PSA ]:
49.36000

[ LogP ]:
1.70180

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
3.01E-07mmHg at 25°C

[ 储存条件 ]:
Desiccate at RT

萘普生钠MSDS

详细MSDS(安全技术说明书)

萘普生钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QJ1047000

CHEMICAL NAME :: 2-Naphthaleneacetic acid, 6-methoxy-alpha-methyl-, sodium salt, L-(-)-

CAS REGISTRY NUMBER :: 26159-34-2

LAST UPDATED :: 199806

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C14-H14-O3.Na

MOLECULAR WEIGHT :: 253.27

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 600 mg/kg/30D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - interstitial nephritis

REFERENCE :: AJDCAI American Journal of Diseases of Children. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1-80(3), 1911-50; V.100- 1960- Volume(issue)/page/year: 142,524,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2464 mg/kg/2W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 36(1,pt2),147,1997 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 20 mg/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 27,505,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 mg/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 38,238,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5640 No. of Facilities: 8 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 239 (estimated) No. of Female Employees: 157 (estimated)

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萘普生钠安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H360

[ 警示性声明 ]:
P201-P308 + P313

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
53-45

[ 危险品运输编码 ]:
UN 3249

[ RTECS号 ]:
QJ1047000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2918990090

萘普生钠合成路线

详细合成路线

萘普生钠上下游产品

萘普生钠上游产品

萘普生钠下游产品

萘普生钠海关

[ 海关编码 ]: 2918990090

[ 中文概述 ]:
2918990090. 其他含其他附加含氧基羧酸（包括酸酐、酰卤化物、过氧化物和过氧酸及该税号的衍生物）. 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 ]:
2918990090. other carboxylic acids with additional oxygen function and their anhydrides, halides, peroxides and peroxyacids; their halogenated, sulphonated, nitrated or nitrosated derivatives. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

萘普生钠文献

Ion-exchange molecularly imprinted polymer for the extraction of negatively charged acesulfame from wastewater samples.

J. Chromatogr. A. 1411 , 23-33, (2015)

Acesulfame is a known indicator that is used to identify the introduction of domestic wastewater into water systems. It is negatively charged and highly water-soluble at environmental pH values. In th...

HPLC method for naproxen determination in human plasma and its application to a pharmacokinetic study in Turkey.

J. Chromatogr. Sci. 52(7) , 584-9, (2014)

A simple high-performance liquid chromatography method has been developed for the determination of naproxen in human plasma. The method was validated on an Ace C18 column using ultraviolet detection. ...

A new analytical method to determine non-steroidal anti-inflammatory drugs in surface water using in situ derivatization combined with ultrasound-assisted emulsification microextraction followed by gas chromatography-mass spectrometry.

Talanta 129 , 552-9, (2014)

Because of the high stability and potential toxic effects of non-steroidal anti-inflammatory drugs (NSAIDs), it is important to closely monitor their concentrations in the environment using a sensitiv...

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