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フィナステリド

フィナステリド 化学構造式
98319-26-7
CAS番号.
98319-26-7
化学名:
フィナステリド
别名:
プロスカル;(-)-N-tert-ブチル-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボキサミド;N-tert-ブチル-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボアミド;プロペシア;フィナストリド;フィナステリド;N-(1,1-ジメチルエチル)-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボアミド;N-tert-ブチル-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボキサミド;フィナステリド (JAN)
英語化学名:
Finasteride
英語别名:
MK-906;Andozac;mk-0906;Fistide;PROSCAR;PROSTIDE;FINASTID;l-652,931;Finastride;Prosteride
CBNumber:
CB9433852
化学式:
C23H36N2O2
分子量:
372.54
MOL File:
98319-26-7.mol

フィナステリド 物理性質

融点 :
253 °C
比旋光度 :
405 -59° (c = 1 in methanol)
沸点 :
576.6±50.0 °C(Predicted)
比重(密度) :
1.065±0.06 g/cm3(Predicted)
貯蔵温度 :
Store at RT
溶解性:
DMSO: 32 mg/mL, soluble
酸解離定数(Pka):
14.17±0.70(Predicted)
外見 :
solid
色:
white to beige
水溶解度 :
insoluble
Merck :
14,4082
InChIKey:
DBEPLOCGEIEOCV-WSBQPABSSA-N
CAS データベース:
98319-26-7(CAS DataBase Reference)
EPAの化学物質情報:
1H-Indeno[5,4-f]quinoline-7-carboxamide, N-(1,1-dimethylethyl)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4aR,4bS,6aS,7S,9aS,9bS,11aR)- (98319-26-7)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  Xn,T,Xi
Rフレーズ  22-61-60-36/37/38
Sフレーズ  36/37/39-45-53-36-26-24/25
WGK Germany  3
RTECS 番号 CL5245000
HSコード  29379000
有毒物質データの 98319-26-7(Hazardous Substances Data)
絵表示(GHS)
注意喚起語 Warning
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 P264, P270, P301+P312, P330, P501
注意書き
P264 取扱い後は皮膚をよく洗うこと。
P264 取扱い後は手や顔をよく洗うこと。
P270 この製品を使用する時に、飲食または喫煙をしないこ と。
P330 口をすすぐこと。

フィナステリド 価格 もっと(22)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01CAY14938
Finasteride
98319-26-7 50mg ¥6000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01CAY14938
Finasteride
98319-26-7 100mg ¥9000 2018-12-26 購入
東京化成工業 F0675 フィナステリド >98.0%(GC)
Finasteride >98.0%(GC)
98319-26-7 200mg ¥17900 2018-12-04 購入
東京化成工業 F0675 フィナステリド >98.0%(GC)
Finasteride >98.0%(GC)
98319-26-7 1g ¥62300 2018-12-04 購入
Sigma-Aldrich Japan 1270402 フィナステリド United States Pharmacopeia (USP) Reference Standard
Finasteride United States Pharmacopeia (USP) Reference Standard
98319-26-7 200mg ¥70900 2018-12-25 購入

フィナステリド 化学特性,用途語,生産方法

用途

フィナステリド(finasteride)は、アメリカメルク社が開発した抗アンドロゲン薬。2型5-α還元酵素を阻害して、男性ホルモンテストステロンがDHT(ジヒドロテストステロン)に転換されるのを抑制する。高用量(5mg/day)で前立腺肥大症?前立腺癌に対して抑制的に作用する。Proscar等の商品名で海外で販売されているが、日本では前立腺の治療薬としては未承認。 低用量(0.2または1mg/day)で、男性型脱毛症(AGA)に対して脱毛抑制効果を認め、プロペシア(Propecia)の商品名で多くの国で発売されている。

効能

抗アンドロゲン薬, 5α還元酵素阻害薬

商品名

フィナステリド (シオノケミカル); フィナステリド (ファイザー); フィナステリド (リョートーファイン); フィナステリド (大興製薬); フィナステリド (富士化学工業); フィナステリド (小林化工); フィナステリド (東和薬品); フィナステリド (武田テバファーマ); フィナステリド (沢井製薬); フィナステリド (辰巳化学); フィナステリド (辰巳化学); プロペシア (MSD)

説明

Finasteride, a novel 4-azasteroid, is a breakthrough in the treatment and control of benign prostatic hyperplasia. Mechanistically, it inhibits the prostatic-specific enzyme 5-alpha reductase, thereby decreasing the conversion of testosterone to dihydrotestosterone. It is reportedly effective in reducing urinary symptoms and prostatic volume and increasing maximal urinary flow rate. Finasteride is also being investigated as a treatment for prostatic cancer.

化学的特性

Off-White Crystalline Powder

Originator

Merck (U.S.A.)

使用

Inhibitor of 5a-reductase, the enzyme which converts testosterone to the more potent androgen, 5a-dihydrotestosterone. Antialopecia agent

使用

Inhibitor of 5α-reductase, the enzyme which converts testosterone to the more potent androgen, 5α-dihydrotestosterone. Antialopecia agent.

使用

anti-androgen, alpha-reductase inhibitor

使用

Treatment of benign prostatic hyperplasia and androgenetic alopecia

定義

ChEBI: An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.

適応症

Finasteride (Proscar) is a 5-reductase inhibitor that blocks the conversion of testosterone to DHT in target tissues. Since DHT is the major intracellular androgen in the prostate, finasteride is effective in suppressing DHT stimulation of prostatic growth and secretory function without markedly affecting libido. It is approved for the treatment of benign prostatic hyperplasia. Although there is usually some regression in the size of the prostate gland following administration of finasteride, clinical response may take 6 to 12 months. If the obstructive symptoms are severe, there is often not enough time to allow this compound to work.The principal adverse effects of finasteride are impotence, decreased libido, and decreased volume of ejaculate. The compound is generally well tolerated in men.

brand name

Proscar

生物活性

Antiandrogen that inhibits type II 5 α reductase (IC 50 = 65 nM). Suppresses the conversion of testosterone to dihydrotestosterone. Reduces prostatic dihydrotestosterone levels and prostate size in vivo . Orally active.

薬物動態学

The mean oral bioavailability of finasteride is 65%, as shown in Table 45.4, and is not affected by food. Approximately 90% of circulating finasteride is bound to plasma proteins. Finasteride has been found to cross the blood-brain barrier, but levels in semen were undetectable (<0.2 ng/mL). Finasteride is extensively metabolized in the liver, primarily via CYP3A4 to two major metabolites: monohydroxylation of the t-butyl side chain, which is further metabolized via an aldehyde intermediate to the second metabolite, a monocarboxylic acid. The metabolites show approximately 20% the inhibition of finasteride for 5α-reductase. The mean terminal half-life is approximately 5 to 6 hours in men between 18 and 60 years of age and 8 hours in men older than 70 years of age. Following an oral dose of finasteride, approximately 40% of the dose was excreted in the urine as metabolites and approximately 57% in the feces. Even though the elimination rate of finasteride is decreased in the elderly, no dosage adjustment is necessary. No dosage adjustment is necessary in patients with renal insufficiency. A decrease in the urinary excretion of metabolites was observed in patients with renal impairment, but this was compensated for by an increase in fecal excretion of metabolites. Caution should be used during administration to patients with liver function abnormalities, because finasteride is metabolized extensively in the liver.

臨床応用

The selective inhibition of the type 2 5α-reductase isozyme produces a rapid reduction in plasma DHT concentration, reaching 65% suppression within 24 hours of administering a 1-mg oral tablet (106). At steady state, finasteride suppresses DHT levels by approximately 70% in plasma and by as much as 85 to 90% in the prostate. The remaining DHT in the prostate likely is the result of type 1 5α-reductase. The mean circulating levels of testosterone and estradiol remained within their physiological concentration range. Long-term therapy with finasteride can reduce clinical significant end points of BPH, such as acute urinary retention or surgery. Finasteride is most effective in men with large prostates. Finasteride has no affinity for the AR and no androgenic, antiandrogenic, estrogenic, antiestrogenic, or progestational effects.

Veterinary Drugs and Treatments

Finasteride may be useful in treating the benign prostatic hypertrophy in canine patients. Because of the drug’s relative expense and the long duration of therapy required to see a response, its usefulness may be limited in veterinary medicine.
It may also be useful in the adjunctive treatment of adrenal disease in ferrets.

フィナステリド 上流と下流の製品情報

原材料

準備製品


フィナステリド 生産企業

Global( 402)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Shanghai Payne Pharmaceutical Technology Co.Ltd
18678586262 021-58123769
info@paynepharm.com China 1355 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21836 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22625 55
PI & PI BIOTECH INC.
18371201331
020-81716319 Sales@pipitech.com CHINA 3048 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 2680 55
Shanghai Zheyan Biotech Co., Ltd.
18017610038
zheyansh@163.com CHINA 3623 58

98319-26-7(フィナステリド)キーワード:


  • 98319-26-7
  • (1S,3aS,3bS,5aR,9aR,9bS,11aS)-9a,11a-dimethyl-N-(2-methylpropyl)-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide
  • 17beta-(n-tert-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one
  • 4-azaandrost-1-ene-17-carboxamide,n-(1,1-dimethylethyl)-3-oxo-,(5-alpha,17-be
  • 4-azaandrost-1-ene-17-carboxamide,n-(1,1-dimethylethyl)-3-oxo-,(5alpha,17beta
  • l-652,931
  • mk-0906
  • n-tert-butyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide
  • 1,(5-ALPHA)-ANDROSTAN-4-AZA-3-ONE-17-BETA-(N-TERT-BUTYL-CARBOXAMIDE)
  • 17BETA-(T-BUTYLCARBAMOYL)-4-AZA-5-ALPHA-ANDROSTEN-3-ONE
  • (5α,17β)-N-(1,1-Dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
  • Andozac
  • Chibrcr-Proscar
  • Firmstid:Prostide
  • Finastride
  • N-(1,1-Dimethylethyl)-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide
  • N-(2-methyl-2-propyl)-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide
  • Finasteride,N-tert-Butyl-3-oxo-4-aza-5α-androst-1-en-17β-carboxamide, MK-906, N-(2-methyl-2-propyl)-3-oxo-4-aza-5α-androst-1-ene-17β-carboxamide
  • Finasteride (200 mg)
  • (5alpha,17beta)-N-(1,1-Dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
  • Finasteride,Proscar
  • (5α,17β)-N-(1,1-DiMethylethyl)-3-oxo-
  • Finasteride API
  • N-(2-METHYL-2-PROPYL)-3-OXO-4-AZA-5ALPHA-ANDROST-1-ENE-17BETA-CARBOXAMIDE
  • MK-906
  • Fistide
  • Prosteride
  • PROSCAR
  • PROSTIDE
  • (1S,2R,7R,10S,11S,14S,15S)-N-tert-butyl-2,15-diMethyl-5-oxo-6-azatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-3-ene-14-carboxaMide
  • 4A,6A,11A-TRIMETHYL-2-OXO-2,4A,4B,5,6,6A,7,8,9,9A,9B,10,11,11A-TETRADECAHYDRO-1H-INDENO[5,4-F]QUINOLINE-7-CARBOXYLIC ACID TERT-BUTYLAMIDE
  • プロスカル
  • (-)-N-tert-ブチル-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボキサミド
  • N-tert-ブチル-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボアミド
  • プロペシア
  • フィナストリド
  • フィナステリド
  • N-(1,1-ジメチルエチル)-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボアミド
  • N-tert-ブチル-3-オキソ-4-アザ-5α-アンドロスタ-1-エン-17β-カルボキサミド
  • フィナステリド (JAN)
  • 酵素阻害剤
  • 男性ホルモン
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