아토바공용
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아토바공용 속성
- 녹는점
- 216-2190C
- 끓는 점
- 535.0±50.0 °C(Predicted)
- 밀도
- 1.349±0.06 g/cm3(Predicted)
- 저장 조건
- 2-8°C
- 용해도
- DMSO: >10mg/mL
- 산도 계수 (pKa)
- 5.01±0.10(Predicted)
- 물리적 상태
- 가루
- 색상
- 노란색
- 최대 파장(λmax)
- 494nm(aq. Buffer)(lit.)
- Merck
- 14,866
- InChIKey
- KUCQYCKVKVOKAY-CTYIDZIISA-N
- CAS 데이터베이스
- 95233-18-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | N | ||
---|---|---|---|
위험 카페고리 넘버 | 50/53 | ||
안전지침서 | 60-61 | ||
유엔번호(UN No.) | 3077 | ||
WGK 독일 | 3 | ||
RTECS 번호 | QJ5616500 | ||
HS 번호 | 29147000 | ||
유해 물질 데이터 | 95233-18-4(Hazardous Substances Data) |
아토바공용 C화학적 특성, 용도, 생산
개요
Atovaquone is an orally active antiprotozoal agent indicated for patients with mild to moderate AIDS-associated Pneumocystis carinii pneumonia who are intolerant to the fist-line therapy of trimethoprim-sulfamethoxazole. It is also under investigation as a treatment for malaria and AIDS-associated toxoplasmosis.화학적 성질
Yellow to Orange Crystalline Solid용도
Atovaquone inhibits the cytochrome bc(1) complex via interactions with the Rieske iron-sulfur protein and cytochrome b in the ubiquinol oxidation pocket. In addition to its use as a treatment for toxoplasmosis, atovaquone has antimalarial properties and prevents pneumocystis pneumonia post-renal transplant.정의
ChEBI: A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.Antimicrobial activity
It is active against erythrocytic, liver and sexual stages of malaria parasites. It shows synergy with proguanil and tetracyclines in vitro. It is also active against Babesia spp. and both tachyzoites and cysts of Tox. gondii. Pn. jirovecii is sensitive in vitro at 0.1–3.0 mg/L and high doses are effective in the rat.원료
Point mutations on parasite cytochrome b, in particular at codon 268, cause resistance and readily occur when the drug is used alone. The rapid selection of resistance led to the development of the synergistic combination with proguanil. Failure of Pn. jirovecii prophylaxis has also been associated with cytochrome b mutations.일반 설명
Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.Atovaquone belongs to the class of naphthoquinones with a broad-spectrum activity against parasitic infections including malaria, toxoplasmosis and Pneumocystis pneumonia. It is a potent antiprotozoal compound which aids in collapsing the mitochondrial membrane potential in a malaria parasite.
Pharmaceutical Applications
A hydroxynaphthoquinone. Available as the trans isomer (which is more active than the cis form) for oral use. It is insoluble in water.Mechanism of action
Atovaquone is thought to produce its antiparasitic action by virtue of its ability to inhibit the mitochondrial respiratory chain. More specifically, atovaquone is a ubiquinone reductase inhibitor, inhibiting at the cytochrome bc1 complex. This action leads to a collapse of the mitochondrial membrane potential. The compound shows stereospecific inhibition, with the trans isomer being more active than the cisisomer.Pharmacokinetics
Oral absorption: PoorCmax 750 mg oral: 27 mg/L (steady state)
Plasma half-life: 70 h
Plasma protein binding: >99%
It is highly lipophilic and is poorly absorbed from the gastrointestinal tract following oral administration. Bioavailability is improved when administered with meals, particularly those with a high fat content. Steady-state plasma concentrations are up to 50% lower in AIDS patients than in asymptomatic HIV-positive cases and the elimination half-life is lower (55 h) in patients with AIDS. The concentration in CSF is <1% of the plasma level. Unlike some other naphthoquinones it is not metabolized by human liver microsomes. Combinations with co-trimoxazole (in HIV patients) and with proguanil plus artesunate in healthy adults did not produce any changes in atovaquone pharmacokinetics.
Clinical Use
Pn. jirovecii pneumonia; alternative therapy for mild to moderate illness (prophylaxis and treatment)Prophylaxis and treatment of malaria in combination with proguanil
It has also been used in cerebral toxoplasmosis in AIDS patients and in a few cases of human babesiosis.
부작용
Most clinical trials of atovaquone alone have involved patients with AIDS in whom adverse effects are often difficult to detect; however, more than 20% reported fever, nausea, diarrhea and rashes. There were limited changes in hepatocellular function. In malaria, in combination with proguanil, there are few reported side effects.신진 대사
Atovaquone is poorly absorbed from the GI tract because of its poor water solubility and high fat solubility, but the absorption can be significantly increased if taken with a fat-rich meal. The drug is highly bound to plasma protein (94%) and does not enter the CNS in significant quantities. It is not significantly metabolized in humans and is exclusively eliminated in feces via the bile.아토바공용 준비 용품 및 원자재
원자재
3-메톡시프로피온산
시클로헥센
사이클로헥세인
1-Cyclohexylethan-1-one
염화알루미늄
1,4-나프토퀴논
과황산암모늄
이황화탄소
중아황산나트륨
아세틸 염화물
2-Chloro-1,4-naphthoquinone
질산 은
준비 용품
아토바공용 공급 업체
글로벌( 422)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei Mojin Biotechnology Co., Ltd | +8613288715578 |
sales@hbmojin.com | China | 12470 | 58 |
Ouhuang Engineering Materials (Hubei) Co., Ltd | +8617702722807 |
admin@hbouhuang.com | China | 3001 | 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 | 21687 | 55 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9340 | 55 |
career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29914 | 58 |
Shaanxi Yikanglong Biotechnology Co., Ltd. | 17791478691 |
yklbiotech@163.com | CHINA | 296 | 58 |
Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 |
alice@crovellbio.com | China | 8829 | 58 |
Xiamen AmoyChem Co., Ltd | +86-592-6051114 +8618959220845 |
sales@amoychem.com | China | 6387 | 58 |
HubeiwidelychemicaltechnologyCo.,Ltd | 18627774460 |
faith@widelychemical.com | CHINA | 742 | 58 |
아토바공용 관련 검색:
C.I. 색소 VI올ET 19 4-클로로페닐 이소시안산 벤즈히드릴클로라이드 트리틸클로라이드 사이클로헥사논 2-히드록시퀴노린
Chlorodimethylphenylsilane
CHLOROPHOSPHONAZO III
Gliquidone
trans,trans-2,4-Undecadienal
Buparvaquone
Quinocetone
Phenylacetone
parvaquone
2-(4'-chloro-2,3,4,5-tetrahydro-[1,1'-biphenyl]-4-yl)-3-hydroxynaphthalene-1,4-dione
4-(4-Chlorophenyl)cyclohexanecarboxylic acid
Atovaquone Impurity 5
Atovaquone-D5