2,4-Diamino-5-(3,4,5-Trimethoxybenzyl)Pyrimidine 甲氧苄氨嘧啶
CAS 738-70-5 MFCD00036761
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信息真实价格透明
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专业采购外包团队在线服务
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分类
- Pharmaceuticals
- {SNA} Antibacterial, Antibiotics, Antibiotics A to Z, Antibiotics T-Z, Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Chemical Structure Class, Core Bioreagents, Folic Acid Metabolism, Inhibits an Enzyme, Interferes with DNA Synthesis, L - Z, Mechanism of Action, Metabolic Pathways, Metabolomics, Pyridines and Pyrimidines,
- {SNA} 1694 Pharmaceuticals & Personal Care Products, APIs & Metabolites, APIs (Active Pharmaceutical Ingredients) & Metabolites, Alphabetical Index of Analytical Standards, Analytical Standards, Analytical/Chromatography, Antibacterial,
- {SNA
产品应用
- An antibacterial agent which selectively inhibits dihydrofolate reductase.
相关文献及参考
- Manius, G.J., et al.: Anal. Profiles Drug Subs., 7, 445 (1978),
- Roth, B., et al.: J. Med. Chem., 23, 379 (1980),
- Brogden, R.N., et al.: Drugs, 23, 405 (1982),
安全信息
GHS Symbol
- P201 Obtain special instructions before use. 使用前获取专门指示。
- P202 Do not handle until all safety precautions have been read and understood. 已阅读并理解所有的安全预防措施之前,切勿操作。
- P203
- P260 Do not breathe dust/fume/gas/mist/vapours/spray. 不要吸入粉尘/烟/气体/烟雾/蒸汽/喷雾。
- P263 Avoid contact during pregnancy/while nursing. 怀孕/哺乳期间避免接触。
- P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
- P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西,喝水或吸烟。
- P273 Avoid release to the environment. 避免释放到环境中。
- P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
- P281 Use personal protective equipment as required. 使用所需的个人防护装备。
- P301+P310
- P301+P312
- P301+P316
- P301+P317
- P308+P313
- P314 Get medical advice/attention if you feel unwell. 获取医疗咨询/就医,如果你觉得不舒服
- P318
- P319
- P321 Specific treatment (see … on this label). 具体治疗(见本标签上的)。
- P330 Rinse mouth. 漱口
- P391 Collect spillage. Hazardous to the aquatic environment 收集对水环境有危害的泄漏物。
- P405 Store locked up. 上锁保管。
- P501 Dispose of contents/container to..… 处理内容物/容器.....
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - woman DOSE/DURATION : 60 mg/kg/10D-I TOXIC EFFECTS : Blood - thrombocytopenia REFERENCE : NZMJAX New Zealand Medical Journal. (New Zealand Medical Assoc., P.O. Box 156, Wellington, New Zealand) V.1- 1900- Volume(issue)/page/year: 106,251,1993
TYPE OF TEST : LD50 - Lethal dose
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TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 90 mg/kg TOXIC EFFECTS : Vascular - BP lowering not characterized in autonomic section REFERENCE : CHTHBK Chemotherapy (Basel). (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.13- 1968- Volume(issue)/page/year: 14,37,1969
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1460 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - acute pulmonary edema Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : NKRZAZ Chemotherapy (Tokyo). (Nippon Kagaku Ryoho Gakkai, 2-20-8 Kamiosaki, Shinagawa-Ku, Tokyo 141, Japan) V.1- 1953- Volume(issue)/page/year: 21,175,1973
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 132 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JCHEEU Journal of Chemotherapy. (Edizioni Riviste Scientifiche, via R. Giuliani, 419, 50141 Florence, Italy) V.1- 1989- Volume(issue)/page/year: 5,400,1993
TYPE OF TEST
TYPE OF TEST : Mutation in microorganisms TEST SYSTEM : Microorganism - not otherwise specified DOSE/DURATION : 50 ug/plate REFERENCE : AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 12,84,1977
TYPE OF TEST : DNA inhibition TEST SYSTEM : Human Lymphocyte DOSE/DURATION : 10 umol/L REFERENCE : BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 26,1593,1977
TYPE OF TEST : Mutation in microorganisms TEST SYSTEM : Bacteria - Salmonella typhimurium DOSE/DURATION : 15 ug/plate REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 188,197,1987
TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Human Lymphocyte DOSE/DURATION : 50 umol/L REFERENCE : BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Par
TYPE OF TEST : Phage inhibition capacity TEST SYSTEM : Bacteria - Escherichia coli DOSE/DURATION : 10 ug/plate REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 43,2819,1983
TYPE OF TEST : Sperm Morphology ROUTE OF EXPOSURE : Unreported TEST SYSTEM : Rodent - rat DOSE/DURATION : 800 mg/kg/8D REFERENCE : JOURAA Journal of Urology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1917- Volume(issue)/page/year: 112,348,1974
TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE : 2250 mg/kg SEX/DURATION : female 11-13 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : ANANAU Anatomischer Anzeiger. (VEB Gustav Fischer Verlag, Postfach 176, Jena DDR-6900, Ger. Dem. Rep.) V.1- 1886- Volume(issue)/page/year: 149,151,1981
- H302 Harmful if swallowed 吞食有害
- H361 Suspected of damaging fertility or the unborn child 怀疑对生育能力或未出生婴儿造成伤害
- H372 Causes damage to organs through prolonged or repeated exposure 长期或频繁接触会损伤器官
- H411 Toxictoaquaticlifewithlonglastingeffects 对水生生物有毒性并具有长期影响。
其他信息
- F:8-10-21
- Sigma Aldrich:738-70-5(sigmaaldrich)
- 参考质量标准:参见《中国兽药典》1990年版 含量(干基)/% ≥99.0 PH 7.5~8.5 干燥失重/% ≤0.5 灼烧残渣/% ≤0.5
- 方法二:三甲氧基苯甲醛经缩合、环合而得。
- 不良反应:甲氧苄啶(简称TMP)毒性较低,常用剂量不良反应少见。由于本品可干扰叶酸代谢,患者可能会出现贫血、白细胞减少及血小板减少等血液系统的反应,多见于剂量过大、疗程过长的情况。故用药期间应勤查血象。本品每日最大用量不应超过0.5g,连续用药时间不应超过1周,血液系统不良反应明显时,可口服叶酸制剂给予纠正。本品不宜与抗肿瘤药物、抗癫痫药物及其他叶酸拮抗剂同时使用;TMP与SMZ或SD合用时偶可致结晶尿。其他不良反应有皮疹及轻度胃肠道反应等。
- MOL 文件:738-70-5.mol
- 乙胺嘧啶类抑菌剂:甲氧苄啶是一种亲脂弱碱性乙胺嘧啶类抑菌剂,又称磺胺增效剂、甲氧苄氨嘧啶、抗菌增效剂、甲氧苄胺嘧啶、甲氧苄嘧啶、三甲氧苄胺嘧啶、三甲氧苄啶,常温下为白色或类白色结晶性粉末,无臭,味苦,在氯仿中略溶,在乙醇或丙酮中微溶,在水中几乎不溶,在冰醋酸中易溶。抗菌谱和磺胺药相似,但抗菌作用较强,对大肠杆菌、奇异变形杆菌、肺炎杆菌、腐生葡萄球菌、多种革兰阳性和阴性细菌有效,但对绿脓杆菌感染无效,最低抑菌浓度常低于10mg/L,单用易引起细菌耐药性,故一般不单独使用,主要与磺胺药组成复方制剂,临床上用于治疗尿路感染、肠道感染、呼吸道感染、菌痢、肠炎、伤寒、脑膜炎、中耳炎、流脑、败血症及软组织感染等。对伤寒、副伤寒疗效不低于氨苄西林,也可与长效磺胺药合用于耐药恶性疟的防治。 甲氧苄啶的抗菌原理是干扰细菌的叶酸代谢。主要作用机制是选择性抑制细菌的二氢叶酸还原酶的活性,使二氢叶酸不能还原为四氢叶酸,而合成叶酸是核酸生物合成的主要组成部分,因此本品阻止了细菌核酸和蛋白质的合成,且甲氧卡啶(TMP)与细菌的二氢叶酸还原酶的结合较之对哺乳类动物酶的结合紧密 5~6万倍。与磺胺药的合用可使细菌的叶酸合成代谢遭到双重阻断,有协同作用,使磺胺药抗菌活性增强,并可使抑菌作用转为杀菌作用,减少耐药菌株。另外本品还可增强多种抗生素(如四环素、庆大霉素等)的抗菌作用。
- 上游原料:乙醇 --> 乙酸乙酯 --> 乙酸 --> 甲醇钠 --> 丙烯腈 --> 硝酸胍 --> 赤血盐 --> 2,3,4—三甲氧基苯甲醛
- 方法一:以三甲氧基苯甲醛为原料,先与甲氧基丙腈缩合生成3'4'5'-三甲氧基-2氰基-3甲氧基丙烯,然后在甲醇/甲醇钠中与硝酸胍环合而得。
- 甲氧苄啶价格(试剂级):更新日期 产品编号 产品名称 包装 价格 2014/06/02 T2286 甲氧苄氨嘧啶 Trimethoprim 25G 649元
- 用途三:新型口服广谱抗菌药物。抗菌谱与磺胺药物相似而效力较强,对多种革兰氏阳性和阴性细菌有效。由于细菌对本品将易产生耐药性,故不宜单独作为抗菌药使用。甲氧苄啶与磺胺药合用可使抗菌作用增强数倍至数十倍。该品主要作磺安类药的增效药。一般按1:5的比例使用。也可作为兽药,治疗禽率大肠肝菌引起的败血症,鸡白痢,禽伤寒,霍乱,呼吸系统继发性细菌感染等。还可用于球虫病的治疗。
- 用途四:新型口服光谱抗菌药物。抗菌谱与磺胺药物相似而效力较强,对多种革兰氏阳性和阴性细菌有效。由于细菌对本品将易产生耐药性,故不宜单独作为抗菌药使用。甲氧苄啶与磺胺药合用可使抗菌作用增强数倍至十倍。该品主要做磺胺类药的增效药。也可作为兽药,治疗禽率大肠杆菌引起的败血症,鸡白痢,禽伤寒,霍乱,呼吸系统继发性细菌感染等。还可用于球虫病的治疗。
- 用途一:抗菌增效药,单独用于呼吸道感染、泌尿道感染、肠道感染等病症
- TCI Shanghai:甲氧苄氨嘧啶 Trimethoprim,>;98.0%(LC)(T)(738-70-5)
- MSDS 信息:Trimethoprim(738-70-5).msds
- 用途二:作为抗菌增效药,也可以治疗家禽细菌感染和球虫病。
- Trimethoprim 是一种抑制细菌的抗生素,主要用于预防和治疗