| CAS: | 103-90-2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 分子式: | C8H9NO2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 分子量: | 151.16 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 沸点: | 273 °C | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 熔点: | 168-172℃ | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 中文名称: |
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| 英文名称: |
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| 性质描述: | 从乙醇中得棱柱体结晶。熔点169-171℃，相对密度1.293(21/4℃)。能溶于乙醇、丙酮和热水，难溶于水，不溶于石油醚及苯。无气味，味苦。饱和水溶液pH值5.5-6.5。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 生产方法: | 对氨基酚乙酰化而得。方法1：将对氨基酚加入稀乙酸中，再加入冰醋酸，升温至150℃反应7h，加入乙酐，再反应2h，检查终点，合格后冷却至25℃以下，甩滤，水洗至无乙酸味，甩干，得粗品。方法2：将对氨基酚、冰醋酸及含酸50%以上的酸母液一起蒸馏，蒸出稀酸的速度为每小时馏出总量的十分之一，待内温升至130℃以上，取样检查对氨基酚残留量低于2.5%，加入稀酸（含量50%以上），冷却结晶。甩滤，先用少量稀酸洗涤，再用大量水洗至滤液接近无色，得粗品。方法1的收率为90%，方法2的收率为90-95%。精制方法：将水加热至近沸时投入粗品。升温至全溶，加入用水浸泡过的活性炭，用稀乙酸调节至pH=4.2-4.6，沸腾10min。压滤，滤液加少量重亚硫酸钠。冷却至20℃以下，析出结晶。甩滤，水洗，干燥得原料药扑热息痛成品。其他的生产方法还有：（1）在冰醋酸中用锌还原对硝基苯酚，同时乙酰化得到对乙酰氨基酚；（2）将对羟基苯乙酮生成的腙，置于硫酸酸性溶液中，加入亚硝酸钠，转位生成对乙酰氨基酚。 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 用途: | 该品为解热镇痛药，国际非专有药名为Paracetamol。它是最常用的非抗炎解热镇痛药，解热作用与阿司匹林相似，镇痛作用较弱，无抗炎抗风湿作用，是乙酰苯胺类药物中最好的品种。特别适合于不能应用羧酸类药物的病人。用于感冒、牙痛等症。对乙酰氨基酚也是有机合成中间体，过氧化氢的稳定剂，照相化学药品。 |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||||||||
| A800442 | MACKLIN | 对乙酰氨基苯酚 | 分析对照品 | 114元/250mg; | 咨询 | ||||||||||||||||||||||||||||||||||
储存：室温 状态：白色结晶粉末 | |||||||||||||||||||||||||||||||||||||||
| A800440 | MACKLIN | 对乙酰氨基苯酚 | 98% | 29元/25g; 48元/100g; 176元/500g; 576元/2.5kg; 2132元/10kg; | 咨询 | ||||||||||||||||||||||||||||||||||
储存：室温 状态：白色晶体或晶体粉末 | |||||||||||||||||||||||||||||||||||||||
| A800441 | MACKLIN | 对乙酰氨基苯酚 | 试剂级, 99.0% | 47元/25g; 95元/100g; 310元/500g; 1095元/2.5kg; 3402元/10kg; | 咨询 | ||||||||||||||||||||||||||||||||||
储存：室温 状态：白色粉末或晶体 | |||||||||||||||||||||||||||||||||||||||
| 508902 | J&K | 4-Acetamidophenol | 98.5%, 选择性COX-2抑制剂 | 264元/250G; 935元/1KG; 3126元/5kg; | 咨询 | ||||||||||||||||||||||||||||||||||
基本信息
产品描述 Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug[1][2][3]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[4]. 靶点（IC50 & Targe） COX-1,113.7μM COX-2,25.8μM 体外研究 In vitro, acetaminophen elicites a 4.4-fold selectivity toward COX-2 inhibition (IC50 113.7 μM for COX-1; IC50 25.8 μM for COX-2). Following oral administration of the drug, maximal ex vivo inhibitions are 56% (COX-1) and 83% (COX-2). Acetaminophen plasma concentrations remaine above the in vitro IC50 for COX-2 for at least 5 h postadministration. Ex vivo IC50 values (COX-1: 105.2 μM; COX-2: 26.3 μM) of acetaminophen compared favorably with its in vitro IC50 values. In contrast to previous concepts, acetaminophen inhibited COX-2 by more than 80%, i.e., to a degree comparable to nonsteroidal antiinflammatory drugs (NSAIDs) and selective COX-2 inhibitors. However, a >95% COX-1 blockade relevant for suppression of platelet function is not achieved[1]. MTT assay shows that Acetaminophen (APAP) in a dose of 50 mM significantly (p<0.001) reduces cell viability to 61.5±6.65%. Interestingly, the significant (p<0.01) increase in cell viability to 79.7±2.47% is observed in the Acetaminophen/HV110 co-treated cells, compared to Acetaminophen treated cells[2]. 体内研究 Administering Acetaminophen (250 mg/kg, orally) to the mice causes significant (p<0.001) liver damage and necrosis of cells as evidenced by the elevated serum hepatic enzymes alanine aminotransferase (ALT), aminotransferase (AST), alkaline phosphatase (ALP), and gamma-glutamyl transferase (γGT) compared with normal group. Conversely, effects of pretreatment with different doses of citral (125, 250, and 500 mg/kg) exhibited a significant (p<0.05) decrease in serum activities of ALT (91.79%, 93.07%, and 95.61%, resp.), AST (93.40%, 91.89%, and 96.52%, resp.), ALP (39.29%, 37.07%, and 59.80%, resp.), and γGT (92.83%, 91.59%, and 93.0%, resp.), when compared to the Acetaminophen group. Similar results were found in pretreatment with SLM on the activity of ALT (95.90%), AST (95.03%), ALP (70.52%), and γGT (92.69%)[3]. 细胞实验 Human hepatoma cell line HepG2 is cultured in low glucose DMEM supplemented with 10% fetal bovine serum (FBS), 100 U/mL Penicillin and 100 μg/mL Streptomycin and 2 mM l-glutamine. The cells are maintained in 75 cm2 flasks at 37°C in a humidified atmosphere containing 5% CO2 and split at 80% confluence every 5 days. Cells are seeded in 24-well plate (2×105 cells) and incubated at 37°C overnight followed by cells pretreatment with complete DMEM containing high glucose concentration in order to downregulate autophagy. After 6 h, cells are treated with different concentrations of postbiotics obtained from Lactobacillus fermentum BGHV110 strain (HV110) in order to select appropriate dose for further experiments. Postbiotic is dissolved in complete DMEM medium and added to the cells in specific final concentration. In all other experiments seeded cells are treated with 50 mM Acetaminophen alone or co-treated with 50 mM Acetaminophen and selected dose of lyophilized HV110. To analyze autophagic flux, simultaneously with treatments, cells are exposed to lysosomotropic agent Chloroquine at a concentration of 25 μM, to inhibit autophagosome-lysosome fusion[2].MCE has not independently confirmed the accuracy of these methods. They are for reference only. 动物实验 Mice[3] Male Swiss mice (30-40 g) are used. The experimental animals are divided into six groups of five animals each. Firstly, each group receive orally during seven days the following treatment: Group I: the mice do not receive any treatment (normal). Group II: the mice receive citral vehicle (0.1% Tween 80 solution). Groups III-V: the mice are pretreated with citral at doses of 125, 250, and 500 mg/kg, respectively. Group VI: the mice are pretreated with the hepatoprotective standard drug Silymarin (SLM) (200 mg/kg). After this time, the animals fasted for 8 h and then receive oral Acetaminophen on the seventh day at a dose of 250 mg/kg in Groups II-VI. Group I orally receive saline that contained 0.1% Tween 80 solution (Acetaminophen vehicle). The stock solution is used as the first concentration of 50 mg/mL and after that is diluted in 0.1% Tween 80 solution to prepare the solutions of 25 and 12.5 mg/mL. After 12 h of Acetaminophen administration, serum samples and liver tissue are collected followed by biochemistry and histological analysis.MCE has not independently confirmed the accuracy of these methods. They are for reference only. 参考文献 [1]. Hinz, B, et al. Acetaminophen (paracetamol) is a selective cyclooxygenase-2 inhibitor in man. FASEB J, 2008. 22(2): p. 383-90. [2]. Dini? M, et al. Lactobacillus fermentum Postbiotic-induced Autophagy as Potential Approach for Treatment ofAcetaminophen Hepatotoxicity. Front Microbiol. 2017 Apr 6;8:594. [3]. Uchida NS, et al. Hepatoprotective Effect of Citral on Acetaminophen-Induced Liver Toxicity in Mice. Evid Based Complement Alternat Med. 2017;2017:1796209. [4]. Rothen JP, et al. Acetaminophen is an inhibitor of hepatic N-acetyltransferase 2 in vitro and in vivo. Pharmacogenetics. 1998 Dec;8(6):553-9 安全信息
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| 987818 | J&K | Paracetamol | 98% | 150元/100MG; | 咨询 | ||||||||||||||||||||||||||||||||||
基本信息
安全信息
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| R12027 | Alfa Aesar | 4-Acetamidophenol; Paracetamol,1000ppm | 880元/1ml; | 咨询 | |||||||||||||||||||||||||||||||||||
安全信息 危险等级 | |||||||||||||||||||||||||||||||||||||||
| 005037 | Fluorochem | 4-Acetamidophenol | 98% | 220元/1g; 308元/25g; 748元/250g; 1848元/1kg; | 咨询 | ||||||||||||||||||||||||||||||||||
基本信息
安全信息
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| HY-66005 | MCE | Acetaminophen,103-90-2,对乙酰氨基酚_MCE(MedChemExpress) | 300元/500 mg; 400元/5 g; 600元/10 g; | 咨询 | |||||||||||||||||||||||||||||||||||
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。 AcetaminophenMCE 国际站：Acetaminophen 品牌：MedChemExpress (MCE) 货号：HY-66005 CAS 号：103-90-2 生物活性：对乙酰氨基酚（扑热息痛）是一种选择性环氧合酶-2 (COX-2) 抑制剂，IC50 为 25.8 μM，是一种广泛使用的解热镇痛药。[1][2][3] 对乙酰氨基酚也是一种强效的肝脏 N-乙酰转移酶 2 (NAT2) 抑制剂。[4] 对乙酰氨基酚可诱导小鼠铁死亡，并导致急性肝损伤。[5] 体外研究(In Vitro)：Acetaminophen 对 COX-2 的抑制选择性为 4.4 倍（COX-1 的 IC50 113.7 μM；COX-2 的 IC50 25.8 μM）。口服该药物后，最大体外抑制率为 56%（COX-1）和 83%（COX-2）。给药后至少 5 小时内，Acetaminophen 血浆浓度仍高于体外 COX-2 的 IC50。Acetaminophen 的 IC50 值（COX-1：105.2 μM；COX-2：26.3 μM）与其体外 IC50 值相比更佳。Acetaminophen 抑制 COX-2 的程度超过 80%，即与非甾体抗炎药 (NSAID) 和选择性 COX-2 抑制剂相当。然而，与抑制血小板功能相关的 COX-1 阻断率 >95% 并未实现[1]。 体内研究(In Vivo)：注意： 请勿仅参考一篇文章来确定实验条件。建议在正式实验前，通过预实验确定最佳实验条件 (动物品系、年龄、剂量、频率及周期、检测时间及指标等)。给小鼠服用 Acetaminophen (250 mg/kg，口服) 会导致肝损伤严重和细胞坏死，表现为血清肝酶丙氨酸氨基转移酶（ALT）、氨基转移酶（AST）升高[3]。 Acetaminophen (300 mg/kg，腹腔注射，单剂量) 通过提高 Fe2+ 和丙二醛 (MDA) 的水平，并降低谷胱甘肽 (GSH) 和谷胱甘肽过氧化物酶 4 (GPX4) 的水平，诱导铁死亡，并在 C57BL/6J 小鼠模型中诱发急性肝脏损伤[5]。 诱导肝脏损伤模型[3] 致病原理 高剂量 Acetaminophen 会导致急性肝损伤。大剂量 Acetaminophen 会导致 N-乙酰对苯醌亚胺 (NAPQI) 水平升高，并可能与肝脏蛋白发生反应，导致肝损伤。 具体造模方法： 小鼠：瑞士小鼠 • 雄性 • (30-40 g)给药方式：250 mg/kg • 口服 • 单剂量 Note (1) 给药 12 小时后，采集血清样本和肝组织，进行生化和组织学分析。(2) Acetaminophen 溶解于含有 0.1% Tween 80 (HY-Y1891) 溶液的生理盐水中。 造模成功指标 组织病理学变化：可见严重坏死区，其特征是大面积坏死，伴有小叶中心静脉充血，存在致密和/或中等程度的多形核细胞浸润，以及肝细胞空泡化。 生化变化：血清肝酶 ALT、AST、ALP 和 γGT 升高；显著增加髓过氧化物酶 (MPO) 活性。 拮抗产品：Citral (HY-N7083) MCE尚未独立确认这些方法的准确性。 仅供参考。 分子量：151.16 Formula：C8H9NO2 性状：固体 颜色：White to off-white 中文名称：对乙酰氨基酚；乙酰氨基酚；扑热息痛；退热净；醋氨酚；对醋氨酚；索密痛；乙酰氨基苯酚；二醋洛尔 运输条件：美国大陆地区的室温；其他地区可能有所不同。 储存方式：室温保存3年 *该产品在现溶液现状态不稳定，建议您用配，即刻使用。 文献引用：MCE 顾客使用本产品发表 73 篇科研文献 提供质量检测报告：Data Sheet、SDS、COA、HNMR、RP-HPLC、LCMS、产品使用指南 产品活性：Acetaminophen (Paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂，IC50 值为 25.8 μM。Acetaminophen 是一种有效的肝 N-乙酰转移酶 2 (NAT2) 抑制剂。Acetaminophen 是广泛使用的解热和止痛剂。Acetaminophen 可以在小鼠体内诱导铁死亡 (ferroptosis)，并造成急性肝损伤。 相关产品：Acetaminophen (Standard) | Acetylcysteine | Acetylcysteine (Standard) | Rapamycin (Standard) | Rapamycin | Rapamycin (GMP Like) | Dimethyl sulfoxide, meets analytical specification of Ch.P. | Rapamycin | Dimethyl sulfoxide | Ferrostatin-1 | Cisplatin | 5-Fluorouracil (Standard) 热门产品线：多肽 | 寡核苷酸 | 天然产物 | 生化试剂 | 荧光染料 Trending products：Peptides | Oligonucleotides | Natural Products | Biochemical Assay Reagents | Fluorescent Dyes MCE 疾病模型: MedChemExpress 整理了大量文献报道的动物品系、周龄、给药剂量、给药途径、造模周期及模型评价信息，并展示部分客户验证与 MedChemExpress 实验验证结果，使科研人员在选择产品的同时能够获得较为完整的实验参考。MedChemExpress 相关造模产品已用于多种公开科研研究，应用案例发表于 Nature Chemical Biology、Cancer Cell、Nature Neuroscience、Gut、Science Translational Medicine 等期刊。 MedChemExpress 重点把控杂质、重金属、内毒素等可能影响动物实验结果的因素，经 NMR、LC-MS、HPLC、手性分析、元素分析及活性检测多维度评价；产品页提供 COA、质检报告、溶解度及动物实验配制信息，使用指南覆盖给药溶液配制与技术支撑，帮助研究从选品顺畅衔接到实验实施。凭借广泛的模型覆盖、丰富的造模选择、文献与实验验证、严格的质量控制及完善的现货和技术支持体系，MedChemExpress 能为不同阶段的疾病研究与药物研发提供稳定、便捷、有实验参考价值的造模解决方案。 参考文献： 品牌介绍:
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| HY-66005R | MCE | Acetaminophen (Standard),103-90-2,对乙酰氨基酚（标准品）_MCE(MedChemExpress) | 250元/25 mg; 400元/50 mg; 600元/100 mg; | 咨询 | |||||||||||||||||||||||||||||||||||
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。 Acetaminophen (Standard)MCE 国际站：Acetaminophen (Standard) 品牌：MedChemExpress (MCE) 货号：HY-66005R CAS 号：103-90-2 产品简介：Acetaminophen (Standard) 是 Acetaminophen 的分析标准品。本产品用于研究及分析应用。Acetaminophen (Paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂，IC50 值为 25.8 μM。Acetaminophen 是一种有效的肝 N-乙酰转移酶 2 (NAT2) 抑制剂。Acetaminophen 是广泛使用的解热和止痛剂。 产品应用：该化合物为分析标准品级别，是含量检测的分析标准品，常用于液相、气相和质谱的定性、定量及方法学研究实验中。 分子量：151.16 Formula：C8H9NO2 性状：固体 颜色：White to off-white 中文名称：对乙酰氨基酚（标准品）；乙酰氨基酚（标准品）；扑热息痛（标准品）；退热净（标准品）；醋氨酚（标准品）；对醋氨酚（标准品）；索密痛（标准品）；乙酰氨基苯酚（标准品）；二醋洛尔（标准品） 运输条件：美国大陆地区的室温；其他地区可能有所不同。 储存方式：请按照分析证书中推荐的条件储存产品。 文献引用：MCE 顾客使用本产品发表 1 篇科研文献 提供质量检测报告：SDS、COA、HNMR、RP-HPLC、MS、产品使用指南 产品活性：Acetaminophen (Standard) 是 Acetaminophen 的分析标准品。本产品用于研究及分析应用。Acetaminophen (Paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂，IC50 值为 25.8 μM。Acetaminophen 是一种有效的肝 N-乙酰转移酶 2 (NAT2) 抑制剂。Acetaminophen 是广泛使用的解热和止痛剂。 相关产品：Acetaminophen | Rapamycin (Standard) | Dimethyl sulfoxide (Standard) | Acetylcysteine (Standard) | Rapamycin | Phorbol 12-myristate 13-acetate (Standard) | Hydrocortisone (Standard) | Acetylcysteine | Rapamycin (GMP Like) | Dexamethasone (Standard) | Rapamycin | Indomethacin (Standard) 热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类 Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides MCE 抑制剂: MedChemExpress 信号通路产品覆盖细胞凋亡、自噬、细胞周期与 DNA 损伤、表观遗传、GPCR/G 蛋白、免疫与炎症、JAK/STAT、MAPK/ERK、膜转运体与离子通道、代谢酶与蛋白酶、神经信号、NF-κB、PI3K/Akt/mTOR、PROTAC、蛋白酪氨酸激酶/受体酪氨酸激酶、干细胞/Wnt、TGF-β/Smad 及维生素 D/核受体等研究方向，为肿瘤、感染、炎症与免疫、神经系统疾病、代谢性疾病、心血管疾病和内分泌研究提供多维度的产品选择，助力客户发表文献超 80,000 篇。 相关产品可根据具体情况提供化学结构、作用靶点、生物活性、纯度、溶解度、体内外研究信息、参考文献及质量分析报告 (COA)等资料。 客户发表文献： 品牌介绍:
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