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Rofecoxib

Rofecoxib 구조식 이미지
카스 번호:
162011-90-7
상품명:
Rofecoxib
동의어(영문):
VIOXX;MK-0966;ROFECOXIB;Rofecoxid;AKOS 92137;Rofecoxib(Vioxx);Rofecoxib (MK0966);Rofecoxib (MK 966);Rofecoxib USP/EP/BP;4-[4-(Methylsulfonyl)phenyl]-3-phenyl-
CBNumber:
CB6327130
분자식:
C17H14O4S
포뮬러 무게:
314.36
MOL 파일:
162011-90-7.mol

Rofecoxib 속성

녹는점
207°C
끓는 점
577.6±50.0 °C(Predicted)
밀도
1.333±0.06 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO: soluble5mg/mL, clear (warmed)
물리적 상태
powder
색상
white to beige
수용성
9mg/L(25 ºC)
Merck
14,8248
CAS 데이터베이스
162011-90-7(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xn
위험 카페고리 넘버 22
WGK 독일 3
RTECS 번호 LU5135000
유해 물질 데이터 162011-90-7(Hazardous Substances Data)
그림문자(GHS):
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 P264, P270, P301+P312, P330, P501
예방조치문구:

Rofecoxib C화학적 특성, 용도, 생산

개요

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.

화학적 성질

Off-White (Pale Yellow) Crystalline Powder

Originator

Merck (US)

용도

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

용도

antipsychotic

용도

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

용도

Rofecoxib has been used in high performance bioaffinity chromatography.

정의

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.

Indications

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.

상표명

Vioxx (Merck).

Biochem/physiol Actions

Rofecoxib is derived from furanone and has the ability to cross human placenta. Along with anti-inflammatory action, it possesses analgesic and antipyretic properties. Cytosolic hepatic enzymes are responsible for the metabolism of rofecoxib. It is known to cause oligohydramnios and ductus arteriosus constrictions. Rofecoxib inhibits the action of CYP1A2 (cytochrome P450 family 1 subfamily A member 2). It might be associated with aseptic meningitis. Rofecoxib is known to ameliorate the risk of colorectal adenoma, but might contribute to toxicity.

Mechanism of action

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.

Pharmacokinetics

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.

Clinical Use

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.

Rofecoxib 준비 용품 및 원자재

원자재

준비 용품


Rofecoxib 공급 업체

글로벌( 241)공급 업체
공급자 전화 팩스 이메일 국가 제품 수 이점
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 26782 60
career henan chemical co
+86-0371-55982848
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

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