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氟灭酸

氟灭酸(Flufenamic Acid,530-78-9)一种止痛和消炎药,用于风湿病。 它具有EC 1.14.99.1(前列腺素-内过氧化物合酶)抑制剂,非甾体类抗炎药,非麻醉性镇痛药和退热药的作用。 它是一种芳香族氨基酸和一种有机氟化合物。 它衍生自二苯胺,邻氨基苯甲酸和(三氟甲基)苯。 它是氟草酸酯的共轭酸。
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
YZM000774-200mg 200mg 99.9% ¥ 0.00 ¥ 0.00 Backorder
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¥ 0.00
YZM000774-100mg 100mg 99.9% ¥ 480.00 ¥ 480.00 1-3天
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中文别名 氟灭酸(Flufenamic Acid,530-78-9)
英文别名 Flufenamic Acid(氟灭酸,530-78-9)
CAS号 530-78-9
Inchi InChI=1S/C14H10F3NO2/c15-14(16,17)9-4-3-5-10(8-9)18-12-7-2-1-6-11(12)13(19)20/h1-8,18H,(H,19,20)
InchiKey LPEPZBJOKDYZAD-UHFFFAOYSA-N
分子式 Molecular Weight C14H10F3NO2
分子量 Formula 281.23
溶解度Solubility Soluble to DMSO
性状 Crystalline Powder or Chunks
储藏条件 Storage conditions Refrigerator
氟灭酸(Flufenamic Acid,530-78-9)毒性:
生物 测试类型 路线 报告剂量(标准化剂量) 影响 参考
guinea pig LD50 oral 925mg/kg (925mg/kg)   Pharmacology: International Journal of Experimental and Clinical Pharmacology. Vol. 11, Pg. 220, 1974.
mouse LD50 intramuscular 500mg/kg (500mg/kg)   Pharmaceutical Chemistry Journal Vol. 17, Pg. 353, 1983.
mouse LD50 intraperitoneal 150mg/kg (150mg/kg)   National Technical Information Service. Vol. AD691-490,
mouse LD50 intravenous 158mg/kg (158mg/kg)   Yakugaku Zasshi. Journal of Pharmacy. Vol. 89, Pg. 1392, 1969.
mouse LD50 oral 490mg/kg (490mg/kg) BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION

BEHAVIORAL: ATAXIA
Oyo Yakuri. Pharmacometrics. Vol. 16, Pg. 1011, 1978.
mouse LD50 subcutaneous 620mg/kg (620mg/kg) BEHAVIORAL: ANTIPSYCHOTIC

GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"
Oyo Yakuri. Pharmacometrics. Vol. 18, Pg. 845, 1979.
rat LD50 intraperitoneal 185mg/kg (185mg/kg) BEHAVIORAL: ATAXIA

BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

LUNGS, THORAX, OR RESPIRATION: RESPIRATORY DEPRESSION
Oyo Yakuri. Pharmacometrics. Vol. 16, Pg. 1011, 1978.
rat LD50 intravenous 98mg/kg (98mg/kg)   Current Medical Research and Opinion. Vol. 4, Pg. 17, 1976.
rat LD50 oral 249mg/kg (249mg/kg)   Archives Internationales de Pharmacodynamie et de Therapie. Vol. 221, Pg. 132, 1976.
rat LD50 subcutaneous 280mg/kg (280mg/kg)   Oyo Yakuri. Pharmacometrics. Vol. 18, Pg. 845, 1979.
rat LD50 subcutaneous 280mg/kg (280mg/kg) GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA"

BEHAVIORAL: ANTIPSYCHOTIC
Oyo Yakuri. Pharmacometrics. Vol. 18, Pg. 845, 1979.
women TDLo oral 2160mg/kg/26W (2160mg/kg) GASTROINTESTINAL: "HYPERMOTILITY, DIARRHEA" Postgraduate Medical Journal. Vol. 62, Pg. 773, 1986.

氟灭酸(Flufenamic Acid,530-78-9)物理性质:
物理属性 单位 温度(摄氏度) 资源
Melting Point 133.5 deg C   EXP
log P (octanol-water) 5.25 (none)   EXP
Water Solubility 9.09 mg/L 25 EXP
Vapor Pressure 1.95E-06 mm Hg 25 EST
Henry's Law Constant 1.84E-10 atm-m3/mole 25 EST
Atmospheric OH Rate Constant 7.70E-11 cm3/molecule-sec 25 EST

氟灭酸(Flufenamic Acid,530-78-9)实验注意事项:
1.实验前需戴好防护眼镜,穿戴防护服和口罩,佩戴手套,避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生,必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储,并交于专业生物废气物处理公司处理,以免造成环境污染
Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
Tag:氟灭酸(MSDS,氟灭酸(蒸汽压,氟灭酸(合成,氟灭酸(标准,氟灭酸(应用,氟灭酸(合成,氟灭酸(沸点,氟灭酸(闪点,氟灭酸(用途,氟灭酸(溶解度,氟灭酸(价格,氟灭酸(作用,氟灭酸(结构式,氟灭酸(用处,氟灭酸(毒理性质,氟灭酸(物理性质
产品说明 氟灭酸(Flufenamic Acid,530-78-9):氟苯那酸是由带有N-(三氟甲基)苯基取代基的邻氨基苯甲酸组成的芳族氨基酸。
IntroductionFlufenamic Acid(530-78-9):Flufenamic acid is an aromatic amino acid consisting of anthranilic acid carrying an N-(trifluoromethyl)phenyl substituent.
Application1氟灭酸(Flufenamic Acid,530-78-9)An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth a
Application2
Application3
Stimulatory Effects of Soluplus? on Flufenamic Acid β-Cyclodextrin Supramolecular Complex: Physicochemical Characterization and Pre-clinical Anti-inflammatory Assessment AAPS PharmSciTe/PMID: 32430787
Additive-Induced Metastable Single Crystal of Mefenamic Acid Pharmaceutical Research 2006/PMID: 16927183
Inhibition of eryptosis and intraerythrocytic growth of Plasmodium falciparum by flufenamic acid Naunyn-Schmiedeberg's Archives of Pharmacology 2006/PMID: 17180616
Modulation of Glutamate and Glycine Transporters by Niflumic, Flufenamic and Mefenamic Acids Neurochemical Research 2009/PMID: 19444608
Aminoethoxydiphenyl Borate and Flufenamic Acid Inhibit Ca2+ Influx Through TRPM2 Channels in Rat Dorsal Root Ganglion Neurons Activated by ADP-Ribose and Rotenone The Journal of Membran/PMID: 21509529

Protection of normal cells from irradiation bystander effects by silica-flufenamic acid nanoparticles

Abstract

The development of a myriad of nanoparticles types has opened new possibilities for the diagnostics and treatment of many diseases, especially for cancer. However, most of the researches done so far do not focus on the protection of normal cells surrounding a tumor from irradiation bystander effects that might lead to cancer recurrence. Gap-junctions are known to be involved in this process, which leads to genomic instability of neighboring normal cells, and flufenamic acid (FFA) is included in a new group of gap-junction blockers recently discovered. The present work explores the use of mesoporous silica nanoparticles MCM-41 functionalized with 3-Aminopropyltriethoxysilane (APTES) for anchoring the flufenamic acid for its prolonged and controlled release and protection from radiation bystander effects. MCM-41 and functionalized samples were structurally and chemically characterized with multiple techniques. The biocompatibility of all samples was tested in a live/dead assay performed in cultured MRC-5 and HeLa cells. HeLa cells cultured were exposed to 50 Gy of gamma-rays and the media transferred to fibroblast cells cultured separately. Our results show that MCM-41 and functionalized samples have high biocompatibility with MCR-5 and HeLa cells, and most importantly, the FFA delivered by these NPs was able to halt apoptosis, one of main bystander effects.


Rabbit dehydrogenase/reductase SDR family member 11 (DHRS11): Its identity with acetohexamide reductase with broad substrate specificity and inhibitor sensitivity, different from human DHRS11

Abstract

Human dehydrogenase/reductase SDR family member 11 (DHRS11) has been recently reported to be an NADP+-dependent 3(17)β-hydroxysteroid dehydrogenase, and its orthologs are predicted in genomic analyses of various animals. Among them, the amino acid sequence of predicted rabbit DHRS11 shares 92% identity with that of human DHRS11 and matches peptide sequences (composed of total 87 amino acids) of rabbit heart acetohexamide reductase (RHAR) previously reported. However, the physiological role of RHAR remains unknown, because its known substrates are only acetohexamide and 1,4-naphthoquinone. To elucidate whether the two rabbit enzymes are identical, we have isolated the cDNA for rabbit DHRS11, which was abundantly detected in the brain, heart, kidney and intestine by RT-PCR. The recombinant rabbit DHRS11 reduced acetohexamide and 1,4-naphthoquinone, and was inhibited by tolbutamide and phenobarbital (RHAR-specific inhibitors), demonstrating its identity with RHAR. Rabbit DHRS11 also reduced α-dicarbonyl compounds, aldehydes and aromatic ketones (acetylbenzenes and acetylpyridines), and exhibited 3(17)β-hydroxysteroid dehydrogenase activity. It was competitively inhibited not only by tolbutamide and phenobarbital, but also more potently by several non-steroidal anti-inflammatory drugs such as diclofenac and sulindac. The broad substrate specificity and inhibitor sensitivity were different from those of human DHRS11, which did not reduce aliphatic aldehydes and aromatic ketones despite its higher 3(17)β-hydroxysteroid dehydrogenase activity, and was insensitive to tolbutamide, phenobarbital and diclofenac. The site-directed mutagenesis of Thr163 and Val200 in human DHRS11 to the corresponding residues (Gly and Leu, respectively) in rabbit DHRS11 suggested that these residues are pertinent to the differences in properties of rabbit and human DHRS11s.

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