포사코나졸
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포사코나졸 속성
- 녹는점
- 170-1720C
- 끓는 점
- 850.7±75.0 °C(Predicted)
- 밀도
- 1.36±0.1 g/cm3(Predicted)
- 인화점
- 9℃
- 저장 조건
- -20°C
- 용해도
- 클로로포름(약간 용해됨), 메탄올(약간 용해됨)
- 산도 계수 (pKa)
- 14.72±0.20(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 베이지색
- optical activity
- [α]/D -24 to -32°, c = 1.0 in chloroform-d
- Merck
- 14,7602
- InChIKey
- RAGOYPUPXAKGKH-XAKZXMRKSA-N
- SMILES
- [C@]1(OC[C@@H](COC2C=CC(N3CCN(C4=CC=C(N5C=NN([C@@H](CC)[C@@H](O)C)C5=O)C=C4)CC3)=CC=2)C1)(CN1N=CN=C1)C1=CC=C(F)C=C1F |&1:0,3,22,25,r|
- CAS 데이터베이스
- 171228-49-2(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | F,T | ||
---|---|---|---|
위험 카페고리 넘버 | 11-23/24/25-39/23/24/25 | ||
안전지침서 | 7-16-36/37-45 | ||
유엔번호(UN No.) | UN1230 - class 3 - PG 2 - Methanol, solution | ||
WGK 독일 | 3 | ||
RTECS 번호 | XZ5481020 | ||
HS 번호 | 3204.90.0000 | ||
유해 물질 데이터 | 171228-49-2(Hazardous Substances Data) |
포사코나졸 C화학적 특성, 용도, 생산
개요
Posaconazole, launched in the UK, is the newest member of the azole class of antifungal agents to reach the market. It is indicated for the treatment and prophylaxis of a range of invasive fungal infections, including aspergillosis,fusariosis, chromoblastomycosis, mycetoma, and coccidiomycosis in patients who are refractory to, or intolerant of, standard therapy with amphotericin B and/or itraconazole. In the US, it is approved for the prophylaxis of invasive Aspergillus and Candida infections in patients 13 years of age who are at high risk of developing these infections due to being severely immunocompromised. Additionally, it is approved for the treatment of oropharyngeal candidiasis. Posaconazole has an expanded spectrum of activity over other members of the azole antifungals. In addition to potent activity against refractory cases of aspergillosis and fluconazole-resistant Candida, it demonstrates activity against Zygomycetes.화학적 성질
White Solid용도
Posaconazole is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM정의
ChEBI: An N-arylpiperazine that consists of piperazine carrying two 4-substituted phenyl groups at positions 1 and 4. A triazole antifungal drug.Antimicrobial activity
The spectrum includes dimorphic fungi (Blast. dermatitidis, Coccidioides spp., Hist. capsulatum, Pen. marneffei, and Spor. schenckii), molds (Aspergillus spp., Mucor spp., Rhizomucor spp. and Rhizopus spp.), some dematiaceous fungi and yeasts (Candida spp. and Cryptococcus spp.).일반 설명
Technetium (99mTc) exametazime is a mixture of unstablelipophilic enantiomers that rapidly cross the blood-brain barrierand is trapped in the tissues. The proposed trapping mechanismfor localization includes reduction by glutathione. Asimilar diffusion and trapping process occurs with autologouslymphocytes in vitro.Exametazime is also known as hexamethylpropyleneamineoxime or HMPAO. The radiolabeled complex is indicated for cerebral perfusion in stroke, but is most commonlyused for the radiolabeling of autologous leukocytesas an adjunct in the localization of intra-abdominal infectionand inflammatory bowel disease.
Each kit includes several components: (a) reaction vialscontaining a mixture of exametazime, stannous chloride,and sodium chloride; (b) vials of 1% methylene blue; (c)vials of phosphate buffer in 0.9% NaCl; and (d) 0.45-μm syringefilters. Product preparation depends on the intendeduse.
Pharmaceutical Applications
A synthetic triazole available for oral administration.Pharmacokinetics
Cmax 200 mg oral: 0.5 mg/L after 4 hPlasma half-life: 35 h
Volume of distribution: 1774 L
Plasma protein binding: >98%
Absorption
Oral absorption is slow. Absorption from the gastrointestinal tract is improved if the drug is given with a high-fat meal. Blood concentrations increase in proportion to dosage up to 800 mg.
Distribution
It is extensively distributed into body tissues.
Metabolism and excretion
It is not as extensively metabolized by the hepatic cytochrome P450 system as other triazole antifungals. More than 70% of an administered dose is eliminated in the feces, predominantly as unchanged drug. The remainder is excreted as glucuronidated derivatives in the urine. Posaconazole is a substrate for intestinal P-glycoprotein,an adenosine triphosphate-dependent plasma membrane transporter responsible for drug efflux from cells. Multiple peaks in blood concentrations have been observed, suggesting that effluxed drug is reabsorbed into the systemic circulation.
Clinical Use
Invasive aspergillosisFusarium infection
Chromoblastomycosis and mycetoma
Coccidioidomycosis
Oropharyngeal candidosis
Prophylaxis of invasive fungal infections in patients at serious risk
With the exception of oropharyngeal candidosis and prophylaxis, use is presently restricted to patients with disease that is refractory to other antifungal drugs, or who are intolerant to them.
부작용
It is generally well tolerated even for long periods. Unwanted effects include gastrointestinal discomfort and mild to moderate, transient abnormalities of liver enzymes. Rare side effects include cholestasis and hepatic failure.포사코나졸 준비 용품 및 원자재
원자재
준비 용품
포사코나졸 공급 업체
글로벌( 703)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Guangzhou TongYi biochemistry technology Co.,LTD | +8613073028829 |
mack@tongyon.com | China | 2996 | 58 |
ENBRIDGE PHARMTECH CO., LTD. | +8613812269233 |
tinayang@enbridgepharm.com | China | 302 | 58 |
AFINE CHEMICALS LIMITED | +86-0571-85134551 |
info@afinechem.com | China | 15394 | 58 |
Shenzhen Monkono Technology Co.,Ltd | +86-17063441314 |
sansbiotech@outlook.com | China | 677 | 58 |
Hebei Chuanghai Biotechnology Co,.LTD | +86-13131129325 |
sales1@chuanghaibio.com | China | 5886 | 58 |
Zhengzhou Anbu Chem Co.,Ltd | +86-0371-88006763; +8615988602810 |
sales@anbuchem.com | China | 3000 | 58 |
Henan Bao Enluo International TradeCo.,LTD | +86-17331933971 +86-17331933971 |
deasea125996@gmail.com | China | 2503 | 58 |
Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 |
Mandy@hangyubiotech.com | China | 10991 | 58 |
Sigma Audley | +86-15937194204 +86-18126314766 |
nova@sh-teruiop.com | China | 491 | 58 |
Shaanxi TNJONE Pharmaceutical Co., Ltd | +8618740459177 |
sarah@tnjone.com | China | 1143 | 58 |
포사코나졸 관련 검색:
트리페닐포스핀 메틸트리페닐포스포늄브로마이드 2-페닐페놀 케토코나졸 디클로로메틸페닐실란 플루코나졸
Miconazole nitrate
Itraconazole
SAPERCONAZOLE
5-Methyl-1H-benzotriazole
1-(4-Aminophenyl)-4-(4-hydroxyphenyl)piperazine
2-[(1S,2S)-1-ethyl-2-bezyloxypropyl]-2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)-1-piperazinyl]phenyl]- 3H-1,2,4-Triazol-3-one,
(5R-cis)-Toluene-4-sulfonic acid 5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-yl)methyltetrahydrofuran-3-ylmethyl ester
Ravuconazole
1,3-PROPANEDIOL, 2-[2-(2,4-DIFLUOROPHENYL)-2-PROPEN-1-YL]-
(S)-4-(2,4-difluorophenyl)-2-(hydroxymethyl)pent-4-en-1-ylisobutyrate
1-((2S,3R)-2-(benzyloxy)pentan-3-yl)-N-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)hydrazine-1-carboxamide
PHENYL {4-[4-(4-HYDROXYPHENYL)PIPERAZIN-1-YL]PHENYL}CARBAMATE