INCB_024360_HNMR_21750_MedChemExpress

Peptides, Inhibitors, AgonistsProduct Data SheetProduct Name: FR194738 free baseCat. No.:GC31434Chemical Name:CHEMICAL PROPERTIESCas No.: 204067-45-8Molecular Formula: C27H37NO2SMolecular Weight: 439.65Storage: PowderSolubility: Soluble in DMSOChemical Structure:BackgroundFR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.In intact HepG2 cells, FR194738 concentration−dependently inhibits the incorporation of [14C]acetate into free cholesterol an d cholesteryl ester, with IC50s of 4.9 and 8.0 nM, respectively. FR194738 induces intracellular [14C]squalene accumulation. FR194738 increases the incorporation of [14C]acetate into squalene, an intermediate of cholesterol synthesis[1]. FR194738 potently inhibits squalene epoxidase (SE) in HepG2 cell homogenate and liver microsomes in dogs and rats. The inhibitory effect of FR194738 in comparison to the HMG−CoA reductase inhibitors, Simvastatin, Fluvastatin and Pravastatin, on cholesterol biosynthesis in HepG2 cells is examined. Among these compounds, FR194738 is the most potent, with an IC50 of 2.1 nM. The IC50s of Simvastatin, Fluvastatin and Pravastatin are 40, 28 and 5100 nM, respectively[2]. FR194738 inhibits hamster liver microsomal squalene epoxidase activity in a concentration−dependent manner with an IC50 of 14 nM[3].Serum lipid levels in hamsters after daily administration of FR194738 and Pravastatin for 10 d are measured. FR194738 reduces the serum levels of total, non high density lipoprotein (HDL) and HDL cholesterol, and triglyceride. Treatment of hamsters with FR194738 increases HMG−CoA reductase activity by 1.3−fold at 32 mg/kg compared to the control group and does not significantly change that at 100 mg/kg[3].References:[1]. Sawada M, et al. Effect of FR194738, a potent inhibitor of squalene epoxidase, on cholesterol metabolism in HepG2 cells. Eur J Pharmacol. 2001 Nov 9;431(1):11-6.[2]. Sawada M, et al. Synthesis and biological activity of a novel squalene epoxidase inhibitor, FR194738. Bioorg Med Chem Lett. 2004 Feb 9;14(3):633-7.[3]. Sawada M, et al. Inhibition of cholesterol synthesis causes both hypercholesterolemia and hypocholesterolemia in hamsters. Biol Pharm Bull. 2002 Dec;25(12):1577-82.Research Update1. Effect of Hydrofluoric Acid Concentration and Etching Time on Bond Strength to Lithium Disilicate Glass Ceramic. Oper Dent. 2017 Nov/Dec;42(6):606-615. doi: 10.2341/16-215-L. Epub 2017 Jul 14. PMID:28708007AbstractThe aim of this study was to evaluate the influence of different concentrations of hydrofluoric acid (HF) associated with varied etching times on the microshear bond strength (μSBS) of a resin cement to a lithium disilicate glass ceramic. Two hundred seventy-five ceramic blocks (IPS e.max Press [EMX], Ivoclar Vivadent), m easuring 8 mm × 3 mm thickness, were randomly distributed into five groups according to the HF concentrations (n=50): 1%, 2.5%, 5%, 7.5%, and 10%.2. Does acid etching morphologically and chemically affect lithium disilicate glass ceramic surfaces? J Appl Biomater Funct Mater. 2017 Jan 26;15(1):e93-e100. doi: 10.5301/jabfm.5000303. PMID:27647389AbstractBACKGROUND: This study evaluated the surface morphology, chemical composition and adhesiveness of lithium disilicate glass ceramic after acid etching with hydrofluoric acid or phosphoric acid.METHODS: Lithium disilicate glass ceramic specimens polished by 600-grit silicon carbide paper were subjected to one or a combination of these surface treatments: airborne particle abrasion with 50-μm alumina (AA), etch ing with 5% hydrofluoric acid (HF) or 36% phosphoric acid (Phos), and application of silane coupling agent (Si).3. Fatigue failure load of feldspathic ceramic crowns after hydrofluoric acid etching at different concentrations. J Prosthet Dent. 2018 Feb;119(2):278-285. doi: 10.1016/j.prosdent.2017.03.021. Epub 2017 May 26. PMID:28552291AbstractSTATEMENT OF PROBLEM: Hydrofluoric acid etching modifies the cementation surface of ceramic restorations, which is the same surface where failure is initiated. Information regarding the influence of hydrofluoric acid etching on the cyclic loads to failure of ceramic crowns is lacking.PURPOSE: The purpose of this in vitro study was to evaluate the influence of different hydrofluoric acid concentrations on the fatigue failure loads of feldspathic ceramic crowns.。

科研热词 机理 抑制 细胞凋亡 数值模拟 黄铁矿 颤振抑制 瓦斯爆炸 抗氧化酶 抑制机理 抑制剂 小麦 大鼠 动物实验 光合作用 一氧化氮 hiv-1整合酶 黄铜矿 黄瓜 高压 铅 金属材料 过氧化氢 载氧体再生 谷胱甘肽 褐变 衰老 织构 细胞周期 粉煤灰 盐胁迫 电沉积 电场时效 生态剂量 玉米 燃烧特性 混凝土 活性氧 氧化损伤 氧化产物 氧化亚铁硫杆菌 氢气 毒性 柯萨奇病毒 显微组织 抗炎 微尺度 徐变 复合作用 土壤酶 吸附 反应机理 去折叠
替来他明 数值模拟 抗氧化酶 抑菌机理 成花 微乳液法 家蝇 复合掺杂 基因表达 反应机理 卵巢 化感作用 分子机理 分化 净光合速率 免疫耐受 克隆 催化还原 催化剂 休眠 代谢酶 一氧化氮 nm23-h1 na+-k+-atpase hiv-1 龙脑香科 鼓泡吸收 黑果黄皮 黏结 黄连 黄菖蒲 黄瓜幼苗 鱼类 高雷诺数 高脂饮食 高脂食物 高能离子 高氯酸铵 高拱坝 高强铝合金 高压直流输电 高k栅介质 髓外浸润 骨髓增生异常综合征 骨骼肌细胞 骨质 马来酸酐 香蕉 风雨振 风险传递 颤振抑制 颗粒污泥 频率响应 颅脑创伤
1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1
2008年 序号 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52

第18卷 第5期 中国药剂学杂志 Vol. 18 No.5 2020年9月 Chinese Journal of Pharmaceutics Sep. 2020 p.244 收稿日期：2019-11-24作者简介：张德广(1985-)，男(汉族)，安徽宣城人，大学专科生, E-mail ***********************；*通信作者：王启帅(1973-)，男(汉族)，江苏泰州人，硕士研究生，主要从事医药研发及生产管理，Tel. 138****6658，文章编号：2617–8117（2020）05–0244–06 DOI:10.14146/ki.cjp.2020.05.002高效液相色谱法测定硼替佐米中异戊醛含量张德广1，李 贞1，刘 霞1，王启帅2*（1. 扬子江药业集团上海海尼药业有限公司，上海 浦东 201318；2. 扬子江药业集团，江苏 泰州 225321）摘 要：目的 建立高效液相色谱法测定硼替佐米原料药中异戊醛含量。

方法 硼替佐米中的异戊醛用 2,4-二硝基苯肼衍生化，采用 Waters symmetry C 18 色谱柱（250 mm × 4.6 mm ，5 µm ），以乙腈（体积分数 0.1% 甲酸）-水（体积分数 0.1% 甲酸）为流动相进行线性梯度洗脱，流速为 1.0 mL•min -1，检测波长为 364 nm ，柱温为 30 ℃。

结果 异戊醛质量浓度在 0.015～2.998 mg•L -1 内与峰面积呈良好线性关系（r = 1.000 0），平均回收率为 101.1%，RSD 为 1.4%。

结论 该方法准确灵敏、线性范围宽，可以用于稳定性过程中潜在基因毒性杂质异戊醛的评估。

关键词：硼替佐米；异戊醛；高效液相色谱；衍生化中图分类号：R94 文献标志码：A多发性骨髓瘤主要是因为骨髓浆细胞异常克隆增殖所致的一种恶性浆细胞病，在造血系统肿瘤中发病率占比约为 13%，且具有临床治疗效果差，治疗后复发率高等特点[1]。

24.755 23.917 23.654 23.565 23.333 23.194 22.929 22.864 22.864 22.864 22.490 22.345 22.333 21.757 21.543 21.543 20.833 20.761 20.614 19.966 19.795 19.547 19.352 18.571 18.571 18.038 17.983 17.983 17.949 17.689 17.689 17.689 17.436 17.313 17.215 16.417 16.238 16.179 16.008 16.008 15.766 15.575 15.518 15.389 15.389 15.389 15.333 15.333 15.280 15.280 15.265 15.253 15.251 15.202
ONCOLOGY CLINICAL NEUROLOGY PLANT SCIENCES BIOCHEMICAL RESEARCH METHODS ASTRONOMY & ASTROPHYSICS MATERIALS SCIENCE, MULTIDISCIPLINARY PHYSICS, MULTIDISCIPLINARY BIOCHEMISTRY & MOLECULAR BIOLOGY CELL BIOLOGY MEDICINE, RESEARCH & EXPERIMENTAL MICROBIOLOGY PHARMACOLOGY & PHARMACY PHYSICS, PARTICLES & FIELDS CHEMISTRY, MULTIDISCIPLINARY PHARMACOLOGY & PHARMACY TOXICOLOGY CHEMISTRY, MULTIDISCIPLINARY CELL BIOLOGY NEUROSCIENCES INFECTIOUS DISEASES IMMUNOLOGY PHYSIOLOGY PHYSICS, MULTIDISCIPLINARY BEHAVIORAL SCIENCES NEUROSCIENCES ONCOLOGY CELL BIOLOGY DEVELOPMENTAL BIOLOGY ECOLOGY CHEMISTRY, MULTIDISCIPLINARY MAபைடு நூலகம்ERIALS SCIENCE, MULTIDISCIPLINARY NANOSCIENCE & NANOTECHNOLOGY GENETICS & HEREDITY MICROBIOLOGY MEDICINE, GENERAL & INTERNAL MICROBIOLOGY ASTRONOMY & ASTROPHYSICS MATERIALS SCIENCE, MULTIDISCIPLINARY BEHAVIORAL SCIENCES NEUROSCIENCES NEUROSCIENCES PSYCHOLOGY CLINICAL NEUROLOGY ECOLOGY EVOLUTIONARY BIOLOGY GENETICS & HEREDITY CHEMISTRY, PHYSICAL PHYSICS, CONDENSED MATTER BIOCHEMISTRY & MOLECULAR BIOLOGY CELL BIOLOGY PSYCHOLOGY MEDICINE, GENERAL & INTERNAL NEUROSCIENCES CARDIAC & CARDIOVASCULAR SYSTEMS