91714-94-2

• 常用中文名：2-(2-氨基-3-(4-溴苯甲酰基)苯)乙酸
• 常用英文名：Bromfenac
• CAS号：91714-94-2
• 分子式：C₁₅H₁₂BrNO₃
• 分子量：334.165
• 相关类别： 信号通路 免疫及炎症 COX
• 发布时间：2018-08-09 19:55:32
• 更新时间：2024-01-02 19:09:04
• 溴芬酸是一种有效的口服活性COX抑制剂,COX-1和COX-2的IC50分别为5.56和7.45 nM。溴芬酸可用于眼部炎症研究[1]。

名称

• 中文名: 溴芬酸钠
• 英文名: bromfenac
• 英文别名: Bromfenacum [Latin]; Bromfenac [INN]; Benzeneacetic acid, 2-amino-3-(4-bromobenzoyl)-; bromfenacum [INN_la]; 2-[2-amino-3-(4-bromobenzoyl)phenyl]acetic acid; bromfenac; [2-Amino-3-(4-bromobenzoyl)phenyl]acetic acid; Bromfenacum; Bromfenaco [Spanish]; Duract; Xibrom; Bromfenaco

物化性质

• 密度: 1.6±0.1 g/cm3
• 沸点: 562.2±50.0 °C at 760 mmHg
• 熔点: -129ºC
• 分子式: C₁₅H₁₂BrNO₃
• 分子量: 334.165
• 闪点: 293.8±30.1 °C
• 精确质量: 333.000061
• PSA: 80.39000
• LogP: 2.72
• 蒸汽压: 0.0±1.6 mmHg at 25°C
• 折射率: 1.663
• 储存条件: 2-8°C

生物活性

• 描述: 溴芬酸是一种有效的口服活性COX抑制剂,COX-1和COX-2的IC50分别为5.56和7.45 nM。溴芬酸可用于眼部炎症研究[1]。
• 相关类别:
  研究领域 >> 感染
  研究领域 >> 炎症/免疫
  信号通路 >> 免疫及炎症 >> COX
• 靶点:

  Human COX-1:5.56 nM (IC50)

  Human COX-2:7.45 nM (IC50)

• 体外研究: 溴芬酸(0-80μg/mL；24小时)可以浓度依赖性方式抑制转化生长因子-β2诱导的HLEC-B3上皮-间充质转化[2]。溴芬酸(80μg/Ml；48小时)抑制转化生长因子-β2诱导的人前囊上皮-间质转化[2]。细胞存活率测定[2]细胞系：转化生长因子-β2处理的人前囊浓度：80μg/mL孵育时间：48小时结果：抑制转化生长因子β2诱导的原代LEC上皮-间充质转化。细胞迁移试验[2]细胞系：HLEC-B3细胞浓度：0、20、40、60和80μg/mL孵育时间：24小时结果：抑制转化生长因子-β2诱导的HLEC-B3细胞的细胞迁移,并抑制上皮-间质转化标记物的过度表达。
• 体内研究: 溴芬酸(0.0032-3.16%；100或200μL；涂抹在背部)在大鼠体内产生显著的抗炎活性,浓度低至0.1%(4小时预处理时间)或0.32%(18小时预处理)。溴芬酸(0.032-3.16%；100μL；擦在爪子上)在大鼠体内产生剂量相关的抗炎活性[3]。溴芬酸(0.032-1.0%；50μL)在直接应用于豚鼠暴露于紫外线的皮肤区域时,其阻断红斑的效力是消炎痛的26倍[3]。溴芬酸(0.0032-0.1%；50μL；每天在未注射的爪子上摩擦4小时,每周5天)会导致大鼠两后肢爪子体积的剂量和时间依赖性减少[3]。溴芬酸(0.32%；50μL；涂抹在腹部)对小鼠ACh攻击的腹部收缩产生显著的阻断作用[3]。溴芬酸(滴眼液；每眼1μL(0.09%)；每天两次；4W)部分减少角膜染色,并在4周时间点变得更慢[4]。动物模型：雄性Sprague-Dawley大鼠(150-250 g)注射卡拉胶[3]剂量：0.0032、0.01、0.032、0-1、0.32、1.0、3.16%(100或200μL)给药：在注射卡拉胶1-72小时前擦到背部。结果：在卡拉胶激发前1、2和4小时以0.32%的浓度施用时,产生显著的抗炎活性。在卡拉胶激发前1或4小时施用是活性的,但在激发前24小时(或更长时间)以0.2%施用时不是活性的。动物模型：雄性注射Salin或BTX-B[4]剂量：1μL(0.09%)/眼给药：滴眼液；每眼1μL(0.09%)；每天两次；4周结果：治疗后4周角膜荧光素染色评分改善。
• 参考文献:

  [1]. Tetsuo Kida, et al. Pharmacokinetics and efficacy of topically applied nonsteroidal anti-inflammatory drugs in retinochoroidal tissues in rabbits. PLoS One. 2014 May 5;9(5):e96481.

  [2]. Xiaobo Zhang, et al. Drug-eluting intraocular lens with sustained bromfenac release for conquering posterior capsular opacification. Bioact Mater. 2021 Jul 23;9:343-357.

  [3]. Nolan JC, et, al. The topical anti-inflammatory and analgesic properties of bromfenac in rodents. Agents Actions. 1988 Aug; 25(1-2): 77-85.

  [4]. Kaevalin Lekhanont, et al. Effects of topical anti-inflammatory agents in a botulinum toxin B-induced mouse model of keratoconjunctivitis sicca. J Ocul Pharmacol Ther. 2007 Feb;23(1):27-34.

MSDS

Material Safety Data Sheet Section1. Identification of the substance Product Name: Bromfenac Synonyms: Section2. Hazards identification Harmful by inhalation, in contact with skin, and if swallowed. Section3. Composition/information on ingredients. Ingredient name:Bromfenac CAS number:91714-94-2 Section4. First aid measures Skin contact:Immediately wash skin with copious amounts of water for at least 15 minutes while removing contaminated clothing and shoes. If irritation persists, seek medical attention. Eye contact:Immediately wash skin with copious amounts of water for at least 15 minutes. Assure adequate flushing of the eyes by separating the eyelids with fingers. If irritation persists, seek medical attention. Inhalation:Remove to fresh air. In severe cases or if symptoms persist, seek medical attention. Ingestion:Wash out mouth with copious amounts of water for at least 15 minutes. Seek medical attention. Section5. Fire fighting measures In the event of a fire involving this material, alone or in combination with other materials, use dry powder or carbon dioxide extinguishers. Protective clothing and self-contained breathing apparatus should be worn. Section6. Accidental release measures Personal precautions: Wear suitable personal protective equipment which performs satisfactorily and meets local/state/national standards. Respiratory precaution:Wear approved mask/respirator Hand precaution:Wear suitable gloves/gauntlets Skin protection:Wear suitable protective clothing Eye protection:Wear suitable eye protection Methods for cleaning up: Mix with sand or similar inert absorbent material, sweep up and keep in a tightly closed container for disposal. See section 12. Environmental precautions: Do not allow material to enter drains or water courses. Section7. Handling and storage Handling:This product should be handled only by, or under the close supervision of, those properly qualified in the handling and use of potentially hazardous chemicals, who should take into account the fire, health and chemical hazard data given on this sheet. Store in closed vessels, refrigerated. Storage: Section8. Exposure Controls / Personal protection Engineering Controls: Use only in a chemical fume hood. Personal protective equipment: Wear laboratory clothing, chemical-resistant gloves and safety goggles. General hydiene measures: Wash thoroughly after handling. Wash contaminated clothing before reuse. Section9. Physical and chemical properties Appearance:Not specified Boiling point:No data No data Melting point: Flash point:No data Density:No data Molecular formula:C15H12BrNO3 Molecular weight:334.2 Section10. Stability and reactivity Conditions to avoid: Heat, flames and sparks. Materials to avoid: Oxidizing agents. Possible hazardous combustion products: Carbon monoxide, nitrogen oxides, hydrogen bromide. Section11. Toxicological information No data. Section12. Ecological information No data. Section13. Disposal consideration Arrange disposal as special waste, by licensed disposal company, in consultation with local waste disposal authority, in accordance with national and regional regulations. Section14. Transportation information Non-harzardous for air and ground transportation. Section15. Regulatory information No chemicals in this material are subject to the reporting requirements of SARA Title III, Section 302, or have known CAS numbers that exceed the threshold reporting levels established by SARA Title III, Section 313. SECTION 16 - ADDITIONAL INFORMATION N/A

安全

• 危害码 (欧洲): Xi
• 海关编码: 2922509090

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%