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ロフェコキシブ

ロフェコキシブ 化学構造式
162011-90-7
CAS番号.
162011-90-7
化学名:
ロフェコキシブ
别名:
ロフェコキシブ;4-[4-(メチルスルホニル)フェニル]-3-フェニル-2(5H)-フラノン;ロフェコキシブ (JAN)
英語化学名:
Rofecoxib
英語别名:
VIOXX;MK-0966;ROFECOXIB;Rofecoxid;AKOS 92137;Rofecoxib(Vioxx);Rofecoxib (MK0966);Rofecoxib USP/EP/BP;4-[4-(Methylsulfonyl)phenyl]-3-phenyl-;4-[4-(MethylSLdfonyl)phenyl]-3-phenyl-2(5H)-furanone
CBNumber:
CB6327130
化学式:
C17H14O4S
分子量:
314.36
MOL File:
162011-90-7.mol

ロフェコキシブ 物理性質

融点 :
207°C
沸点 :
577.6±50.0 °C(Predicted)
比重(密度) :
1.333±0.06 g/cm3(Predicted)
貯蔵温度 :
2-8°C
溶解性:
DMSO: soluble5mg/mL, clear (warmed)
外見 :
powder
色:
white to beige
水溶解度 :
9mg/L(25 ºC)
Merck :
14,8248
CAS データベース:
162011-90-7(CAS DataBase Reference)
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
Rフレーズ  22
WGK Germany  3
RTECS 番号 LU5135000
有毒物質データの 162011-90-7(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

ロフェコキシブ 価格 もっと(6)

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) W01W0118-0333 ロフェコキシブ 98.0+% (HPLC)
Rofecoxib 98.0+% (HPLC)
162011-90-7 100mg ¥12400 2021-03-23 購入
東京化成工業 R0206 ロフェコキシブ >98.0%(GC)
Rofecoxib >98.0%(GC)
162011-90-7 250mg ¥15400 2021-03-23 購入
東京化成工業 R0206 ロフェコキシブ >98.0%(GC)
Rofecoxib >98.0%(GC)
162011-90-7 1g ¥46000 2021-03-23 購入
Sigma-Aldrich Japan SML0613 ≥98% (HPLC)
Rofecoxib ≥98% (HPLC)
162011-90-7 50mg ¥54720 2021-03-23 購入
Sigma-Aldrich Japan SML0613 ≥98% (HPLC)
Rofecoxib ≥98% (HPLC)
162011-90-7 10mg ¥11600 2021-03-23 購入

ロフェコキシブ 化学特性,用途語,生産方法

外観

白色~黄色、結晶性粉末~粉末

溶解性

ジメチルスルホキシド溶状:試験適合

用途

シクロオキシゲナーゼ2 (COX-2)選択的阻害剤です。抗炎症・鎮痛 作用を示します。長期使用による心血管リス クの増加が確認されています。

効能

鎮痛薬, 抗炎症薬, シクロオキシゲナーゼ2阻害薬

説明

Rofecoxib ts a non-steroidal anti-inflammatory drug (NSAID) launched in Mexico, its first market, for the management of acute pain and the treatment of osteoarthritis (OA) and primary dysmenorrhea. Rofecoxib can be obtained by several different ways; one example is by arylation of a 4-bromofuranone with a phenylboronic acid under Suzuki conditions. Rofecoxib is a highly selective inhibitor of COX-2, the inducible isoform of cyclooxygenase and therefore exhibits a potent antiinflammatory activity without concomitant gastric or renal toxicities linked to the non-specific COX-1/2 inhibitors. In several clinical studies in patients with knee or hip osteoarthritis, Rofecoxib was evaluated at 12.5-50 mg doses once daily: it demonstrated efficacy for all primary and secondary endpoints at doses considerably weaker than those for classical non-specific NSAIDs, with good tolerance and less adverse effects. Selective COX-2 inhibitors potentially have a large spectrum of activity including new indications such as Alzheimer's disease, colorectal cancer, irritable bowel disease or urinary incontinence.

化学的特性

Off-White (Pale Yellow) Crystalline Powder

Originator

Merck (US)

使用

A selective cyclooxygenase-2 (COX-2) inhibitor. Use as an anti-inflammatory, analgesic.

使用

antipsychotic

使用

Labeled Rizatriptan, intended for use as an internal standard for the quantification of Rizatriptan by GC- or LC-mass spectrometry.

定義

ChEBI: A butenolide that is furan-2(5H)-one that is substituted by a phenyl group at position 3 and by a p-(methylsulfonyl)phenyl group at position 4. A selective cyclooxygenase 2 inhibitor, it was used from 1999 to 2004 for the tr atment of ostoarthritis, but was withdrawn following concerns about an associated increased risk of heart attack and stroke.

適応症

Rofecoxib is approved for the treatment of osteoarthritis, dysmenorrhea, and acute pain. The most common adverse reactions to rofecoxib are mild to moderate GI irritation (diarrhea, nausea, vomiting, dyspepsia, abdominal pain). Lower extremity edema and hypertension occur relatively frequently (about 3.5%). It is not metabolized by CYP2C9, so rofecoxib should not be subject to some of the interactions seen with celecoxib. However, its metabolism is increased by the coadministration of rifampin, which acts as a nonspecific inducer of hepatic metabolism.

brand name

Vioxx (Merck).

作用機序

Rofecoxib is excreted primarily in the urine (72%) as metabolites. Less than 1% is excreted in the urine as unchanged drug, whereas approximately 14% is excreted in the feces as unchanged drug. Although the metabolism of rofecoxib has not been fully determined, the microsomal cytochrome P450 system appears to play only a minor role—a major difference in the metabolic routes of rofecoxib and celecoxib. The major metabolic route appears to form reduction of the dihydrofuranone ring system by cystolic enzymes to the to cis- and trans- dihydro derivatives. Also isolated is the glucuronide of a hydroxy derivative that results from CYP2C9 oxidative metabolism. None of the isolated metabolites of rofecoxib possess pharmacological activity as COX-1 or COX-2 inhibitors.

薬物動態学

Rofecoxib has been synthesized by a number of synthetic routes that have been summarized elsewhere. It was the second selective COX-2 inhibitor to be marketed. Rofecoxib is well absorbed from the GI tract on oral administration, with peak plasma levels generally being attained within 2 to 3 hours of dosing. Bioavailability averages 93% following administration of a single dose. The area under the plasma concentration–time curve is increased in patients older than 65 years compared to younger adults and is increased slightly in black and Hispanic patients compared with white patients, but the difference is not considered to be clinically significant.

臨床応用

Rofecoxib was indicated for the relief of the signs and symptoms of osteoarthritis, for the management of acute pain in adults, and for the treatment of primary dysmenorrhea.

ロフェコキシブ 上流と下流の製品情報

原材料

準備製品


ロフェコキシブ 生産企業

Global( 237)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
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 497 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26751 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29954 58
Shandong chuangyingchemical Co., Ltd.
18853181302
sale@chuangyingchem.com CHINA 5917 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 37282 58
Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63726 58
Shenzhen Excellent Biotech Co., Ltd.
13480692018
ramyan@ex-biotech.com;sale@ex-biotech.com CHINA 955 58
HENAN BON INDUSTRIAL CO.,LTD
0371-55170695
info@hnbon.com CHINA 26742 58
Shaanxi Dideu Medichem Co. Ltd
13772537765
029-88380327 1010@dideu.com CHINA 3993 58

162011-90-7(ロフェコキシブ)キーワード:


  • 162011-90-7
  • 4-[4-(MethylSLdfonyl)phenyl]-3-phenyl-2(5H)-furanone
  • 4-[4-(Methylsulfonyl)phenyl]-3-phenyl-
  • Rofecoxib(Vioxx)
  • Rofecoxib (MK0966)
  • Rofecoxid
  • ROFECOXIB
  • MK-0966
  • VIOXX
  • AKOS 92137
  • 4-[4-(METHYLSULFONYL)-PHENYL]-3-PHENYL-2(5H)-FURANONE
  • 4-[4-(methylsulfonyl)phenyl]-3-phenylfuran-2(5h)-one
  • Rofecoxib, MK-0966, 4-[4-(methylsulfonyl)-phenyl]-3-phenyl-2(5H)-furanone
  • 2(5H)-Furanone, 4-4-(methylsulfonyl)phenyl-3-phenyl-
  • Rofecoxib USP/EP/BP
  • 4-(4-methanesulfonylphenyl)-3-phenyl-2,5-dihydrofuran-2-one
  • ロフェコキシブ
  • 4-[4-(メチルスルホニル)フェニル]-3-フェニル-2(5H)-フラノン
  • ロフェコキシブ (JAN)
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