Raltegravir
|
|
Raltegravir 속성
- 녹는점
- 216 °C(Solv: isopropanol (67-63-0))
- 밀도
- 1.46±0.1 g/cm3(Predicted)
- 저장 조건
- -20°C Freezer
- 용해도
- DMSO(약간 용해됨), 메탄올(매우 소량)
- 산도 계수 (pKa)
- 4.50±1.00(Predicted)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 흰색~밝은 베이지
- CAS 데이터베이스
- 518048-05-0(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
유해 물질 데이터 | 518048-05-0(Hazardous Substances Data) |
---|
그림문자(GHS): | ||||||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
신호 어: | Warning | |||||||||||||||||||||
유해·위험 문구: |
|
|||||||||||||||||||||
예방조치문구: |
|
Raltegravir C화학적 특성, 용도, 생산
개요
Joining maraviroc as a unique approach to battling HIV-1, raltegravir, an inhibitor of HIV-1 integrase, represents the first in its class to be developed and launched as a combination treatment with other antiretroviral agents (NRTIs, NNRTIs, and PIs). HIV-1 integrase is essential for replication of the virus as a virally encoded enzyme that integrates the viral DNA into the genome of the host cell. Inhibition of HIV-1 integrase prevents the two-step process of endonucleolytic removal of the terminal dinucleotide from each 3′end of the viral DNA followed by the covalent integration of the viral DNA, at these modified 3′ends, into the host DNA, thereby representing a viable intervention in the viral life cycle. In vitro, raltegravir inhibited the strand transfer activity of HIV-1 integrase with an IC50 of 2–7nM with > 1,000-fold selectivity over other phosphoryltransferases. In addition, its in vitro IC95 for HIV-1 in 10% fetal bovine serum and 50% human serum was 19 and 33 nM, respectively. Raltegravir was well tolerated with no dose-related toxicities and a safety profile comparable to placebo. The most common clinical adverse events were diarrhea, nausea, vomiting, fatigue, headache, flushing, pruritus, and injection-site reactions.용도
Raltegravir (MK-0518, Isentress) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.원료
Several characteristic mutations leading to typical amino acid exchanges have been characterized in cell culture studies and confirmed in clinical trial participants with virological failure while receiving raltegravir in combination with other antiretrovirals. Virological failure has generally been associated with mutations at one of three residues – Y143, Q148 or N155 – usually in combination with at least one other mutation.Pharmaceutical Applications
Formulated as the potassium salt for oral administration.Pharmacokinetics
Oral absorption: Not known/availableCmax 400 mg twice daily: c. 2.17 mg/L
Plasma half-life: c. 9 h
Volume of distribution: Not known/available
Plasma protein binding: c. 83%
Absorption and distribution
It may be administered without regard to food. There are few data regarding its capacity to penetrate into genital secretions or breast milk. A study of 25 HIV-infected individuals receiving raltegravir as a component of combination antiretroviral therapy found that 24 had detectable levels and that 50% of these reached a level exceeding the 95% inhibitory concentration reported to inhibit HIV-1 strains fully susceptible to integrase inhibition.
Metabolism and excretion
It is not a substrate, and does not appear to inhibit or induce the cytochrome P450 enzyme complex. It is primarily metabolized through hepatic glucuronidation mediated by the UGT-1A1 enzyme. It is excreted in the feces (51%) and the urine (32%) as unaltered compound and its glucuronide. There are no recommended dose adjustments for weight, sex and race, or for hepatic or renal insufficiency. The pharmacokinetic handling in children has not been determined.
Clinical Use
Treatment of HIV infection (in combination with other antiretroviral drugs)부작용
Its toxicity profile to date is remarkably benign. Clinical trial participants experienced similar types and frequencies of adverse events as those receiving placebo. The most frequently reported adverse events were nausea, diarrhea and headache and were mostly mild to moderate in intensity. Myopathy, rhabdomyolysis and elevations of creatinine phosphokinase have been noted in a few trial participants and it should be used cautiously in combination with drugs associated with muscle toxicity.Raltegravir 준비 용품 및 원자재
원자재
5-Methyl-1,3,4-oxadiazole-2-carbonyl chloride
2-(1-AMINO-1-METHYLETHYL)-N-(4-FLUOROBENZYL)-5-HYDROXY-1-METHYL-6-OXO-1,6-DIHYDROPYRIMIDINE-4-CARBOXAMIDE
준비 용품
Raltegravir 공급 업체
글로벌( 267)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hubei Ipure Biology Co., Ltd | +8613367258412 |
ada@ipurechemical.com | China | 10326 | 58 |
Henan Tengmao Chemical Technology Co. LTD | +8615238638457 |
salesvip2@hntmhg.com | China | 415 | 58 |
Sigma Audley | +86-18336680971 +86-18126314766 |
nova@sh-teruiop.com | China | 525 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29797 | 60 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21691 | 55 |
Shanghai Yingrui Biopharma Co., Ltd. | +86-21-33585366 - 03@ |
sales03@shyrchem.com | CHINA | 738 | 60 |
career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29914 | 58 |
Jinan Chenghui-Shuangda Chemical Co.,Ltd | +86-531-58897082 |
ericqiao@jnchsd.com | CHINA | 158 | 58 |
TianYuan Pharmaceutical CO.,LTD | +86-755-23284190 13684996853 |
sales@tianpharm.com | CHINA | 304 | 58 |
Biochempartner | 0086-13720134139 |
candy@biochempartner.com | CHINA | 967 | 58 |
Raltegravir 관련 검색:
아크릴산메틸 쿠레톡심메틸 염화벤질 벤설프론 메틸 메틸파라벤 디하이드로미르세놀 염화트리메틸벤질암모늄 염화트리에틸벤질암모늄 티오판산-메틸 나트륨-N-라로일사코신산 브롬화 메틸 메틸 파라싸이온(메틸 파라티온)
Raltegravir Potassium Salt,Raltegravir potassium
METHYL THIOPHENE-2-CARBOXYLATE
CHLOROPHOSPHONAZO III
Raltegravir Diketo Methoxy Impurity
Raltegravir EP impurity C
Raltegravir Diketo Ethoxy Impurity