布洛芬钠盐

布洛芬钠盐用途

布洛芬(±)-布洛芬钠是一种口服活性选择性COX-1抑制剂,IC50值为13μM。布洛芬钠抑制细胞增殖、血管生成和诱导细胞凋亡。布洛芬钠是一种非甾体抗炎剂和一氧化氮(NO)供体。布洛芬钠可用于研究疼痛、肿胀、炎症、感染、免疫学、癌症[1][2][5][8]。

布洛芬钠盐名称

[ CAS 号 ]:
31121-93-4

[ 中文名 ]:
布洛芬钠

[ 英文名 ]:
ibuprofen sodium salt

[中文别名 ]:

苯乙酸,A-甲基-4-(2-甲基丙基)-,钠盐

[英文别名 ]:

EINECS 250-477-6
Sodium ibuprofen
sodium 2-[4-(2-methylpropyl)phenyl]propanoate
p-Isobutylhydratropic acid sodium salt
2-(4'-isobutylphenyl)propionic acid,sodium salt
Sodium 2-(4-isobutylphenyl)propionate
Hydratropic acid,p-isobutyl-,sodium salt
Ibuprofen sodium salt
Ibuprofen sodium
(RS)-ibuprofen sodium

布洛芬钠盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> COX

研究领域 >> 神经疾病

[ 靶点 ]

COX-1:13 μM (IC50)

COX-2:370 μM (IC50)

[体外研究]

布洛芬钠(24小时)抑制COX-1和COX-2活性,IC50值分别为13μM和370μM[1]。布洛芬钠(500μM,48小时)抑制细胞增殖和血管生成,并诱导AGS细胞(腺癌胃细胞系)凋亡[2]。布洛芬钠(500μM,48小时)下调Akt、VEGF-A、PCNA、Bcl2、OCT3/4和CD44基因的转录,但上调AGS细胞中野生型P53和Bax基因的RNA水平[2]。布洛芬钠(500μM,24小时)在囊性纤维化(CF)细胞模型和原发性CF鼻上皮细胞中恢复微管重构、微管依赖性细胞内胆固醇转运,并诱导微管延伸至细胞外周[3]。布洛芬钠(500μM,24小时)通过光敏化过程增强MCF-7细胞和MDA-MB-231细胞中UV诱导的细胞死亡[4]。细胞存活率测定[2]细胞系：AGS细胞浓度：100-1000μM孵育时间：24小时,48小时结果：抑制AGS细胞存活率,IC50值为630μM(台盼蓝染色,24小时)、456微米(中性红染色,24 h)、549微米(台盼兰染色,48小时)和408μM(中性红测定,48小时)。

[体内研究]

布洛芬钠(以动物饲料喂养,300mg/kg,14天)在产后乳腺癌模型中降低总体肿瘤生长并增强抗肿瘤免疫特征,而无不良自身免疫反应[5]。布洛芬钠(皮下注射,60 mg/kg,第二天持续15天)可降低慢性奥沙利铂诱导的周围神经病变大鼠模型中的神经病变风险[6]。布洛芬钠(口服给药,20 mg/kg,每12小时一次,共5剂)可减少肌肉生长(平均肌纤维横截面积),而不影响冈上肌腱对运动的适应性调节[7]。布洛芬钠(口服给药,35 mg/kg,每日两次)减轻慢性肺部感染大鼠模型中对铜绿假单胞菌的炎症反应[8]。动物模型：PPBC(产后)的同基因(D2A1)原位Balb/c小鼠模型[5]剂量：300 mg/kg,每日14天给药：以动物饲料喂养(添加到粉碎的标准食物中,混合干燥,然后与水混合,制成食物颗粒并彻底干燥)。结果：抑制肿瘤生长,减少未成熟单核细胞的存在,增加T细胞的数量。增强Th1相关细胞因子以及促进T细胞的肿瘤边界积聚。动物模型：奥沙利铂诱导的周围神经病变[6]剂量：60 mg/kg,连续15天,第二天给药：皮下注射结果：感觉神经传导速度(SNCV)降低。

[参考文献]

[1]. Noreen Y, et al. Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. J Nat Prod. 1998 Jan;61(1):2-7.

[2]. Hassan Akrami, et al. Inhibitory effect of ibuprofen on tumor survival and angiogenesis in gastric cancer cell. Tumour Biol. 2015 May;36(5):3237-43.

[3]. Sharon M Rymut, et al. Ibuprofen regulation of microtubule dynamics in cystic fibrosis epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L317-27.

[4]. Emmanuelle Bignon, et al. Ibuprofen and ketoprofen potentiate UVA-induced cell death by a photosensitization process. Sci Rep. 2017 Aug 21;7(1):8885.

[5]. Nathan D Pennock, et al. Ibuprofen supports macrophage differentiation, T cell recruitment, and tumor suppression in a model of postpartum breast cancer. J Immunother Cancer. 2018 Oct 1;6(1):98.

[6]. Thomas Krøigård, et al. Protective effect of ibuprofen in a rat model of chronic oxaliplatin-induced peripheral neuropathy. Exp Brain Res. 2019 Oct;237(10):2645-2651.

[7]. Sarah Ilkhanipour Rooney, et al. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model. Am J Sports Med. 2016 Sep;44(9):2237-45.

[8]. M W Konstan, et al. Ibuprofen attenuates the inflammatory response to Pseudomonas aeruginosa in a rat model of chronic pulmonary infection. Implications for antiinflammatory therapy in cystic fibrosis. Am Rev Respir Dis. 1990 Jan;141(1):186-92.

布洛芬钠盐物理化学性质

[ 密度 ]:
1.029g/cm3

[ 沸点 ]:
319.6ºC at 760 mmHg

[ 熔点 ]:
75-77ºC

[ 分子式 ]:
C₁₃H₁₇NaO₂

[ 分子量 ]:
228.26300

[ 闪点 ]:
216.7ºC

[ 精确质量 ]:
228.11300

[ PSA ]:
40.13000

[ LogP ]:
1.73850

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents

[ 水溶解性 ]:
H2O: 100 mg/mL, may be clear to slightly hazy

布洛芬钠盐MSDS

详细MSDS(安全技术说明书)

布洛芬钠盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MU6641000

CHEMICAL NAME :: Hydratropic acid, p-isobutyl-, sodium salt

CAS REGISTRY NUMBER :: 31121-93-4

LAST UPDATED :: 198910

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C13-H17-O2.Na

MOLECULAR WEIGHT :: 228.29

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 gm/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

布洛芬钠盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
MU6641000

[ 海关编码 ]:
2916399090

布洛芬钠盐合成路线

详细合成路线

布洛芬钠盐上下游产品

布洛芬钠盐上游产品

布洛芬钠盐下游产品

布洛芬钠盐海关

[ 海关编码 ]: 2916399090

[ 中文概述 ]:
2916399090 其他芳香一元羧酸. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 丙烯酸、丙烯酸盐或酯应报明包装

[ Summary ]:
2916399090 other aromatic monocarboxylic acids, their anhydrides, halides, peroxides, peroxyacids and their derivatives VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

布洛芬钠盐文献

The advantages and limitations of the analgesics available for control of postoperative pain after a dental procedure.

SAAD Dig. 29 , 70-81, (2013)

Enhanced longevity by ibuprofen, conserved in multiple species, occurs in yeast through inhibition of tryptophan import.

PLoS Genet. 10(12) , e1004860, (2014)

The common non-steroidal anti-inflammatory drug ibuprofen has been associated with a reduced risk of some age-related pathologies. However, a general pro-longevity role for ibuprofen and its mechanist...

Pegylation improves the pharmacokinetics and bioavailability of small-molecule drugs hydrolyzable by esterases: a study of phospho-Ibuprofen.

J. Pharmacol. Exp. Ther. 351(1) , 61-6, (2014)

Esterase hydrolysis of drugs can accelerate their elimination, thereby limiting their efficacy. Polyethylene glycol (PEG) covalently attached to drugs (pegylation) is known to improve the efficiency o...

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