다루나비르
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다루나비르 속성
- 녹는점
- 74-760C
- 밀도
- 1.34±0.1 g/cm3(Predicted)
- 저장 조건
- -20°C
- 용해도
- DMSO에 용해됨(>25mg/ml)
- 산도 계수 (pKa)
- 11.43±0.46(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 베이지색
- 안정성
- 제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
WGK 독일 | 3 | ||
---|---|---|---|
유해 물질 데이터 | 206361-99-1(Hazardous Substances Data) |
다루나비르 C화학적 특성, 용도, 생산
개요
Darunavir is the latest weapon in the arsenal of agents to combat human immunodeficiency virus type 1(HIV-1). As an HIV-1 protease inhibitor, its mechanism of action involves blocking the cleavage of the gag and gag–pol polyproteins into functional proteins essential for the production of infectious progeny virus; the result is the production of immature, noninfectious viral particles. Compared to predecessor HIV protease inhibitors, darunavir retains activity against resistant stains, a critical factor with the continual emergence of multidrug- resistant (MDR) mutants. Despite experiencing a 13-fold reduction in binding to MDR HIV-1 protease, this binding is 1.5 orders of magnitude tighter than the first-generation protease inhibitors. Furthermore, darunavir exhibits less than a 10-fold decrease in susceptibility in cell culture against 90% of 3309 clinical isolates resistant to amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir, and tipranavir. In contrast, darunavir-resistant viruses display limited susceptibility to only tipranavir, suggesting limited cross-resistance between these two protease inhibitors. To avoid the issues of the peptide-based protease inhibitors, darunavir has evolved from a structure-based design effort to minimize peptidic features and reduce molecular weight and complexity.화학적 성질
White Amorphous Solid정의
ChEBI: An N,N-disubstituted benzenesulfonamide bearing an unsubstituted amino group at the 4-position, used for the treatment of HIV infection. A second-generation HIV protease inhibitor, darunavir was designed to form robust interactions with the protease enzyme from many strains of HIV, including those from treatment-experienced patients with multiple resistance mutations to other protease inhibitors.원료
Darunavir is less affected than other protease inhibitors by mutations to resistance, but subgroups with more than 10 cumulative mutations show a >10-fold (median value) decrease in susceptibility. The major resistance mutations occur at positions 50 (150V), 54 (I50M/L), 76 (L76V) and 84 (I84V) of the protease gene.Pharmaceutical Applications
A synthetic compound formulated as the ethanolate for oral use in combination with ritonavir.Pharmacokinetics
Oral absorption: c. 82%Cmax 600 mg once daily + ritonavir 100 mg twice daily: c. 6500 μg/L
Cmin 600 mg oral + ritonavir 100 mg twice daily: c. 3578 μg/L
Plasma half-life: c. 15 h
Volume of distribution: c. 131 L
Plasma protein binding: c. 95%
A single 600 mg dose given orally in combination with ritonavir 100 mg every 12 h increased the systemic exposure of darunavir approximately 14-fold. The relative bioavailability is 30% lower when administered with food in the presence of low-dose ritonavir. Distribution into human CSF, semen or breast milk has not yet been determined.
At least three oxidative metabolites, mediated predominantly through CYP3A4, have been identified in humans; all are at least 10-fold less active than the parent compound against HIV. Around 80% and 14% of the dose is found in the feces and urine, respectively. It should be used with caution in mild–moderate hepatic impairment and avoided in patients with more severe impairment.
Clinical Use
Treatment of HIV infection (in combination with other antiretroviral drugs)부작용
In phase III studies the most common adverse events were diarrhea, nausea, headache and nasopharyngitis. Patients coinfected with hepatitis B or C did not have a higher incidence of adverse events.다루나비르 준비 용품 및 원자재
원자재
준비 용품
다루나비르 공급 업체
글로벌( 326)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Henan Fengda Chemical Co., Ltd | +86-371-86557731 +86-13613820652 |
info@fdachem.com | China | 20293 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21667 | 55 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9357 | 55 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32836 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29888 | 58 |
SHANDONG ZHI SHANG CHEMICAL CO.LTD | +86 18953170293 |
sales@sdzschem.com | China | 2931 | 58 |
HubeiwidelychemicaltechnologyCo.,Ltd | 18627774460 |
faith@widelychemical.com | CHINA | 742 | 58 |
BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 |
sales@chemdad.com | China | 39916 | 58 |
Shaanxi Dideu Medichem Co. Ltd | 18192627656 |
1012@dideu.com | China | 3002 | 58 |
다루나비르 관련 검색:
푸란
Darunavir N-β-D-Glucuronide
FURO[3,4-B]FURAN-2(3H)-ONE, TETRAHYDRO-4-METHOXY-, (3AS,4S,6AR)-
BIS THF HNS Derivative 3
Darunavir Impurity 19
1-epi-Darunavir
(1R,2S)-Darunavir
Citalopram
Donepezil
4-Hydroxy Darunavir
[(3R,3aS,6aR)-Hydroxyhexahydrofuro[2,3-β]furanyl Succinimidyl Carbonate
tert-Butyl [(1S,2R)-1-benzyl-2-hydroxy-3-[isobutyl[(4-nitrophenyl)sulfonyl]amino]propyl]carbamate
Darunavir ethanolate
(3R,3αS,6αR)-Hexahydrofuro[2,3-β]furan-3-yl-4-nitrophenyl carbonate
4-AMINO-N-[(2R,3S)-3-AMINO-2-HYDROXY-4-PHENYLBUTYL]-N-ISOBUTYLBENZENE-1-SULFONAMIDE
Darunavir-D9
2-hydroxyethyl 2-hydroxyethyl-carbamate
Darunavir