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分类

• {SNA} Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology, Enzyme Inhibitors, Enzyme Inhibitors by Type, Enzymes, Inhibitors, and Substrates, F, Substrate Analogs
• Alphabetic, Analytical Standards, Analytical/Chromatography, Bioactive Small Molecules, Cell Biology, Chromatography, Clinical Standards, F, FA - FL, Hormones, Life Sciences Standards, Market Segments, Neats and Solutions, Pharmacology Standards, Standards for Food and Beverage Analysis, Standards for Pharma Clinical Forensic & Veterinary Analysis
• {Chemicalbook} 药物: 其它药物: 其它药物

产品应用

• Inhibitor of 5?-reductase, the enzyme which converts testosterone to the more potent androgen, 5?-dihydrotestosterone.

相关文献及参考

• [2]. Yun DK, et, al. Finasteride Increases the Expression of Hemoxygenase-1 (HO-1) and NF-E2-Related Factor-2 (Nrf2) Proteins in PC-3 Cells: Implication of Finasteride-Mediated High-Grade Prostate Tumor Occurrence. Biomol Ther (Seoul). 2013 Jan;21(1):49-53.
• [3]. Sirinarumitr K, et, al. Effects of finasteride on size of the prostate gland and semen quality in dogs with benign prostatic hypertrophy. J Am Vet Med Assoc. 2001 Apr 15;218(8):1275-80.
• Koronkowski, M.J., et al.: Pharmacotherapy, 13, 309 (1993),
• McConnell, J.D., et al.: N. Engl. J. Med., 338, 557 (1998),
• Merck 14 ,4082
• Tenover, J.L., et al.: Clin. Ther., 19, 243 (1997),
• [1]. Flores E, et, al. Steroid 5alpha-reductase inhibitors. Mini Rev Med Chem. 2003 May;3(3):225-37.
• [1]. Flores E, et, al. Steroid 5alpha-reductase inhibitors. Mini Rev Med Chem. 2003 May;3(3):225-37.
• [2]. Yun DK, et, al. Finasteride Increases the Expression of Hemoxygenase-1 (HO-1) and NF-

安全信息

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 418 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Gastrointestinal - ulceration or bleeding from stomach
   Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
   KSRNAM Kiso to Rinsho.

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Skin and Appendages - dermatitis, other (after systemic exposure)
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 28,4091,1994

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 372 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - ataxia
   Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 28,4091,1994

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 486 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - ataxia
   Lungs, Thorax, or Respiration - respiratory depression
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 28,4091,1994

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 3400 mg/kg
SEX/DURATION            : multigeneration
TOXIC EFFECTS :
   Reproductive - Maternal Effects - parturition
REFERENCE :
   TJADAB Teratology, The International Journal of Abnormal Development. (Alan
   R. Liss, Inc., 41 E. 11th St., New York, NY 10003)  V.1-    1968-
   Volume(issue)/page/year: 42,91,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 6720 mg/kg
SEX/DURATION            : male 12 week(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
   resorbed implants per total number of implants)
REFERENCE :
   REPTED Reproductive Toxicology.  (Pergamon Press Inc., Maxwell House,
   Fairview Park, Elmsford, NY 10523)  V.1-    1987-  Volume(issue)/page/year:
   5,337,1991

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 1500 mg/kg
SEX/DURATION            : female 6-20 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Paternal Effects - other effects on male
REFERENCE :
   TJADAB Teratology, The International Journal of Abnormal Development. (Alan
   R. Liss, Inc., 41 E. 11th St., New York, NY 10003)  V.1-    1968-
   Volume(issue)/page/year: 42,483,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 3360 mg/kg
SEX/DURATION            : male 12 week(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Fertility - male fertility index (e.g. # males impregnating
   females per # males exposed to fertile nonpregnant females)
REFEREN

其他信息

• 上游原料:碳酸钠 --> 高锰酸钾 --> 叔丁醇 --> 三苯基膦 --> 乙二醇 --> 环己酮 --> 氢氧化钾溶液 --> 异丙醇铝 --> 3-甲氧基丙酸 --> 二氧化铂 --> 碘酸钠 --> 孕烯醇酮 --> 2,2'-二硫二吡啶
• MOL 文件:98319-26-7.mol
• 治疗男性型脱发药物:非那雄胺也是一种5α–还原酶的特异性抑制剂，属抗性激素类药，它能阻止睾酮转换为二氢睾酮，从而减少双氢睾酮的合成，降低头皮毛囊和血清中双氢睾酮的含量，使已经受抑的毛囊乳头生发功能恢复，促进头发生长并防止继续脱发，非那雄胺是目前美国食品与药品管理局FDA批准的惟一用于治疗男性型脱发的口服药品，推荐剂量为一次1mg。
• 治疗前列腺增生:非那雄胺 是我国治疗前列腺增生和前列腺炎的一种基础药物，它是合成的4–氮甾体激素化合物，属抗性激素药物，可选择性抑制5α–还原酶，使睾酮转化成5α–双氢睾酮(DHT)的过程变阻，前列腺细胞内雄性激素水平下降，血清中的前列腺特异抗原降低，增大的前列腺体积缩小，尿流率增加，从而减轻患者症状，达到治疗前列腺增生的目的。该药的作用特点是能选择性地阻断雄激素对前列腺的刺激作用，却很少影响男子的性功能。 前列腺增生又叫前列腺肥大，它导致膀胱颈部和后尿道受压迫，引起尿路梗阻以及其他症状和并发症，使患者深感痛苦，多发于50岁以上的男性人群。
• Sigma Aldrich:98319-26-7(sigmaaldrich)
• 用途二:5α-还原酶抑制剂，可抑制睾酮转化为二氢睾酮。用于良性前列腺增生症的治疗。
• 非那雄胺价格(试剂级):更新日期 产品编号 产品名称 包装 价格 2011/04/16 F0675 非那甾胺 Finasteride 200MG 800元 2011/04/16 F0675 非那甾胺 Finasteride 1G 4000元
• 用途一:用于治疗男子前列腺肥大及秃发等病症
• 方法一:以孕烯醇酮为原料。先和吡啶作用，再和甲醇钠反应得3-羟基-5-雄甾烯-17β-羧酸甲酯(Ⅲ)。再和异丙醇铝在甲苯和环己酮中，回流。过滤，洗涤，干燥，减压浓缩。加入石油醚，于5℃搅拌，抽滤得氧化产物(Ⅳ)，收率74.6%。该氧化产物和95%乙醇及10%氢氧化钾溶液，在氮气保护下回流。减压蒸去乙醇后，用6mol几盐酸调至Ph值约为3。抽滤，滤饼用水洗至中性，干燥得水解产物(V)，收率96.4%。水解产物溶于叔丁醇中，搅拌下加入无水碳酸钠的水溶液，回流下滴加高碘酸钠和高锰酸钾的水溶液，加毕回流。冷却，过滤。滤液减压蒸去大部分叔丁醇后，冰浴下用6mol/L盐酸调至Ph值约为2。乙酸乙酯提取，提取液用饱和氯化钠洗，干燥。减压蒸干，乙酸乙酯重结晶得开环产物(Ⅵ)，收率66%。在冰浴冷却下，往乙二醇中通入氨气，加入开环产物，缓慢升至180℃反应。冷却，加水，用6mol／I。盐酸调至Ph值约为2。滤集固体，水洗至中性，用二甲基甲酰胺重结晶，得环合产物(Ⅶ)，收率62.1%。该环合产物和二氧化铂、醋酸及少量高氯酸，在85℃和常压下氢化。滤去催化剂后，减压浓缩至干。残留物用二甲基甲酰胺重结晶，得氢化产物(Ⅷ)，收率92.9%。该氢化产物和三苯基膦、甲苯及2，2’-二吡啶二硫化物(DPDS)混合，室温搅拌。柱层析分离得吡啶硫化物(Ⅸ)，收率79.0%。该硫化物和无水四氢呋喃及叔丁胺，室温搅拌过夜，加入二氯甲烷，用2mol/L盐酸和饱和氯化钠洗，干燥，减压浓缩。残留物用乙酸乙酯重结晶，得酰胺产物(X)，收率77.1%。该酰胺和苯亚硒酸酐及氯苯一起，回流并缓慢蒸出溶剂和生成的水。柱层析分离，粗品用乙酸乙酯重结晶，得白色的非那雄胺晶体，收率52.3％，熔点253～255℃。