Febuxostat

Febuxostat 구조식 이미지
카스 번호:
144060-53-7
상품명:
Febuxostat
동의어(영문):
FBX;Uloric;Febuxostat Impurity;2-(3-cyano-4-isobutoxyphenyl);TMX 67;CS-1598;Tei-6720;NSC63871;Febrista;Adenuric
CBNumber:
CB4841564
분자식:
C16H16N2O3S
포뮬러 무게:
316.37
MOL 파일:
144060-53-7.mol
MSDS 파일:
SDS

Febuxostat 속성

녹는점
238-239°(dec.)
끓는 점
536.6±60.0 °C(Predicted)
밀도
1.31±0.1 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태
가루
산도 계수 (pKa)
2.48±0.10(Predicted)
색상
흰색에서 황백색까지
Merck
14,3948
InChI
InChI=1S/C16H16N2O3S/c1-9(2)8-21-13-5-4-11(6-12(13)7-17)15-18-10(3)14(22-15)16(19)20/h4-6,9H,8H2,1-3H3,(H,19,20)
InChIKey
BQSJTQLCZDPROO-UHFFFAOYSA-N
SMILES
S1C(C(O)=O)=C(C)N=C1C1=CC=C(OCC(C)C)C(C#N)=C1
CAS 데이터베이스
144060-53-7(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
RTECS 번호 XJ3675310
HS 번호 2934.10.2000
그림문자(GHS): GHS hazard pictograms
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 GHS hazard pictograms P264, P270, P301+P312, P330, P501
예방조치문구:
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P301+P312 삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P330 입을 씻어내시오.
P501 ...에 내용물 / 용기를 폐기 하시오.
NFPA 704
0
2 0

Febuxostat C화학적 특성, 용도, 생산

개요

Febuxostat, a selective xanthine oxidase inhibitor, was launched for the chronic management of hyperuricemia in patients with gout. Hyperuricemia is defined as a serum uric acid concentration exceeding the limit of solubility. It predisposes affected persons to gout, a disease characterized by the formation of crystals of monosodium urate or uric acid from supersaturated fluids in joints and other tissues. Crystal deposition is asymptomatic, but it is revealed by bouts of joint inflammation. If left untreated, further crystals accumulate in joints and can form deposits known as tophi. A major aim in gout management is the long-term reduction of serum uric acid concentrations below saturation levels, as this results in crystal dissolution and eventual disappearance.
Febuxostat is a nonpurine derivative with higher potency and selectivity than allopurinol for inhibiting xanthine oxidase. It completely inhibits human xanthine oxidase activity in the lung cancer cell line A549, whereas the activities of other enzymes involved in purine or pyrimidine metabolism (e.g., purine nucleoside phosphorylase, adenosine deaminase, and pyrimidine nucleoside phosphorylase) are affected by<4%.

화학적 성질

Crystalline Solid

물리적 성질

Febuxostat has low solubility. It is almost insoluble in acidic conditions, slightly soluble in neutral conditions, and slightly more soluble in alkaline conditions. It is not suitable for making injections, but it can be taken orally because of its high oil-water partition coefficient and strong ability to cross cell membranes.

용도

Febuxostat is a new generation xanthine oxidase inhibitor developed by Tejin Co. (Japan,) used clinically for for long-term treatment of hyperuicemia (gout,) a new and highly effective non-purine selective inhibitor of xanthine oxidase. 40-120 mg/day febuxostat was proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout. It is not recommended for gout patients without hyperuricemia.

제조 방법

Febuxostat can be synthesized in a multistep sequence from 2,4-dicyanophenol, starting with the alkylation of the phenolic hydroxyl group with isobutyl bromide and potassium carbonate, followed by treatment with thioacetamide in hot dimethyl formamide to yield 3-cyano-4-isobutoxythiobenzamide. Cyclization of the thioamide group with 2-chloroacetoacetic acid ethyl ester in refluxing ethanol affords 2-(3-cyano-4-isoutoxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester, which is hydrolyzed with sodium hydroxide to produce febuxostat.

일반 설명

Febuxostat is a potent, non-purine compound, which inhibits the expression of cytokines/chemokines. It has also been reported to inhibit LPS-induced TNF-α, VCAM-1, MMP9 and MCP-1 expression.

Clinical Use

Fabuxostat was discovered by Teijin Pharmaceuticals and licensed to TAP Pharmaceuticals (which is currently part of Takeda Pharmaceuticals) and was approved in the U.S. for the treatment of hyperuricemia in patients with gout. It is a once-daily non-purine based agent with potent inhibitory activity against xanthine oxidase. The safety profile of the drug also does not require dose adjustment for patients with mild to moderate renal or hepatic impairment. Febuxostat is the first new agent cleared for this indication in 40 years.

부작용

The incidence of adverse events such as dizziness, diarrhea, headache, and nausea with febuxostat was similar to allopurinol. Febuxostat is contraindicated in patients being treated with the xanthine oxidase substrates such as azathioprine, mercaptopurine, and theophylline.

Mode of action

Xanthine oxidase is the main enzyme promoting uric acid production. It works by non-competitively blocking the molybdenum pterin center, which is the active site of xanthine oxidase. Through highly selective inhibition of oxidized and reduced xanthine oxidase, Febuxostat can reduce the synthesis of uric acid, decreasing its concentration and effectively treating gout. Through liver metabolism, Xanthine oxidase does not rely on renal excretion, so patients with moderate to severe liver and kidney dysfunction do not need to reduce dosages. Febuxostat is a non-purine XOR inhibitor, so it is very safe.

Febuxostat 준비 용품 및 원자재

원자재

준비 용품


Febuxostat 공급 업체

글로벌( 844)공급 업체
공급자 전화 이메일 국가 제품 수 이점
SHANDONG BOYUAN PHARMACEUTICAL CO., LTD.
+86-0531-69954981 +8615666777973
dwyane.wang@boyuanpharm.com China 211 58
shan dong Fengjin Pharmaceutical company
+8615066764791
liangfulin@fengjin-pharma.com China 8 58
Wuhan Boyuan Import & Export Co., LTD
+86-15175982296 15175982296;
Mike@whby-chem.com China 983 58
Hebei Mojin Biotechnology Co., Ltd
+86-13288715578 +86-13231137666
sales@hbmojin.com China 12409 58
Zibo Hangyu Biotechnology Development Co., Ltd
+86-15965530500 +86-15965530500
nickzhang@hangyubiotech.com China 11001 58
Anhui Ruihan Technology Co., Ltd
+8617756083858
daisy@anhuiruihan.com China 994 58
Shanghai Affida new material science and technology center
+86-15081010295 +86-15081010295
jan@oudaxin.com China 332 58
hebei hongtan Biotechnology Co., Ltd
+852-97803454 +86-17731935328
sales01@chemcn.cn China 233 58
Capot Chemical Co.,Ltd.
571-85586718 +8613336195806
sales@capotchem.com China 29797 60
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
sales01@cooperate-pharm.com CHINA 1811 55

Febuxostat 관련 검색:

Copyright 2019 © ChemicalBook. All rights reserved