Stavudine
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Stavudine 속성
- 녹는점
- 159-160°C
- 알파
- D25 -39.4° (c = 0.701 in water); D20 -46.1° (c = 0.7 in water)
- 밀도
- 1.374±0.06 g/cm3(Predicted)
- 굴절률
- -46 ° (C=0.69, H2O)
- 저장 조건
- -20°C
- 용해도
- 물에 용해되고, 에탄올(96%)에 조금 용해되며, 염화메틸렌에 약간 용해됩니다. 다형성(5.9)을 보여줍니다.
- 물리적 상태
- Solid
- 산도 계수 (pKa)
- 9.47±0.10(Predicted)
- 색상
- 하얀색
- 수용성
- 21&C에서 5~10g/100mL
- BCS Class
- 1,3
- 안정성
- 안정적인. 타기 쉬운. 강한 산화제와 호환되지 않습니다.
- InChIKey
- XNKLLVCARDGLGL-JGVFFNPUSA-N
- CAS 데이터베이스
- 3056-17-5(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | Xi | ||
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위험 카페고리 넘버 | 36/37/38 | ||
안전지침서 | 26-36 | ||
WGK 독일 | 2 | ||
RTECS 번호 | XP2075000 | ||
HS 번호 | 29349990 | ||
유해 물질 데이터 | 3056-17-5(Hazardous Substances Data) | ||
독성 | LD50 oral in rat: 4gm/kg |
그림문자(GHS): | |||||||||||||||
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신호 어: | Warning | ||||||||||||||
유해·위험 문구: |
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예방조치문구: |
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Stavudine C화학적 특성, 용도, 생산
개요
Stavudine, a dideoxynucleoside analog of thymidine, has been introduced in the U.S.A. for the treatment of late-stage AIDS patients who are refractory to other AIDS treatments. Similar as other currently available agents for AIDS treatment such as zidovudine (AZT), didanosine, and zalcitabine, the anti-HIV activity of these 2'3'- dideoxynucleosides is ascribed to the inhibitory effect of their corresponding 5'- triphosphates against the HlVsncoded RNAdependent DNA polymerase (reverse transcriptase). While some of these drugs have rapid development of drug resistance, stavudine is active against AZT-resistant HIV strains. It has a favorable pharmacokinetic profile with more complete and less variable oral absorption than AZT and didanosine and has a bioavailability of 80-90%.화학적 성질
Colourless solid용도
Stavudine (Zidovudine EP Impurity A) is used as an antiviral. A reverse transcriptase inhibitor.Indications
Stavudine (d4T, Zerit) is a thymidine nucleoside analogue that is active against HIV-1 and HIV-2. It is approved for the therapy of HIV infection as part of a multidrug regimen and is also used for postexposure prophylaxis.정의
ChEBI: A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptaseAntimicrobial activity
Stavudine is active against HIV-1, HIV-2 and HTLV-1.원료
Resistance to stavudine is identical to that seen for zidovudine. Mutations at positions 41, 67 and 70, and positions 210, 215 and 219 (the ‘thymidine analog mutations’) of the reverse transcriptase genes are associated with diminished antiretroviral efficacy.일반 설명
Stavudine, 2'3'-didehydro-2'-deoxythymidine (D4T, Zerit), isan unsaturated pyrimidine nucleoside that is related to thymidine.The drug inhibits the replication of HIV by a mechanismsimilar to that of its close congener, AZT.Stavudine is bioactivatedby cellular enzymes to a triphosphate.Stavudine is available as capsules for oral administration.The drug is acid stable and well absorbed (about 90%) followingoral administration. Stavudine has a short half-life(1–2 hours) in plasma and is excreted largely unchanged(85%–90%) in the urine.As with ddC, the primary doselimitingeffect is peripheral neuropathy.
Stavudine isrecommended for the treatment of adults with advancedHIV infection who are intolerant of other approved therapiesor who have experienced clinical or immunological deteriorationwhile receiving these therapies.
공기와 물의 반응
Water soluble.반응 프로필
Stavudine is sensitive to heat. Incompatible with strong oxidizing agents .위험도
Moderately toxic by ingestion.화재위험
Literature sources indicate that Stavudine is combustible.Pharmaceutical Applications
An analog of thymidine formulated for oral administration.Pharmacokinetics
Oral absorption: 86%Cmax 40 mg twice daily: 0.54 mg/L
Plasma half-life: 1.4 h
Volume of distribution: 0.66 L/kg
Plasma protein binding: <5%
Absorption and distribution
It is rapidly absorbed with or without food. CNS penetration is moderate. The estimated semen:plasma ratio is >1. It is secreted into breast milk.
Metabolism and excretion
The metabolic fate in humans has not been elucidated. Renal elimination accounts for approximately 40% of overall clearance at a rate almost twice that of endogenous creatinine, indicating glomerular filtration and active tubular secretion. Clearance decreases as creatinine clearance decreases and the dosage should be adjusted in patients with reduced renal function. Pharmacokinetics are not significantly altered in patients with hepatic impairment.
Clinical Use
Treatment of HIV infection in adults and children부작용
The adverse effects with which stavudine is most frequently associated are headache, diarrhea, skin rash, nausea, vomiting, insomnia, anorexia, myalgia, and weakness. Peripheral neuropathy consisting of numbness, tingling, or pain in the hands or feet is also common with higher doses of the drug. Significant elevation of hepatic enzymes may be seen in approximately 10 to 15% of patients. Lactic acidosis occurs more frequently with stavudine than with other NRTIs. Viral resistance to stavudine may develop, and cross-resistance to zidovudine and didanosine may occur.주의 사항
Stavudine possesses several clinically significant interactionswith other drugs. Although hydroxyurea enhancesthe antiviral activity of stavudine and didanosine,combination therapy that includes stavudine anddidanosine, with or without hydroxyurea, increases therisk of pancreatitis. Combinations of stavudine and didanosineshould not be given to pregnant women becauseof the increased risk of metabolic acidosis.Zidovudine inhibits the phosphorylation of stavudine;thus, this combination should be avoided.Stavudine 준비 용품 및 원자재
원자재
Epoxy
포타슘터셔리부톡사이드
티미딘
메탄설포닐 클로라이드
초산에틸
Anhydrous pyridine
Uridine, 5-methyl-, 2',3',5'-triacetate
Uridine, 2',3'-dideoxy-2'-iodo-5-methyl-, 5'-(2,2-dimethylpropanoate)
Thymidine, 2',3'-didehydro-3'-deoxy-5'-O-[(1,1-dimethylethyl)diphenylsilyl]- (9CI)
((2S,5R)-5-(2,4-Dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2,5-dihydrofuran-2-yl)methyl acetate
(R)-5-(TERT-부틸디페닐실록시메틸)디하이드로-2(3H)푸라논
5-Methyluridine
1-(3,5-ANHYDRO-2-DEOXY-BETA-D-THREO-PENTOFURANOSYL)-5-METHYLPYRIMIDINE-2,4(1H,3H)-DIONE
[(2S,5R)-5-(5-methyl-2,4-dioxo-pyrimidin-1-yl)-2,5-dihydrofuran-2-yl]methyl benzoate
5'-O-TRITYL-2',3'-DEHYDROTHYMIDINE
2,3'-안히드로티미딘
트리부틸아민
오소 포름산 메틸
준비 용품
Stavudine 공급 업체
글로벌( 513)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 |
sales@hbmojin.com | China | 12459 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21670 | 55 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29897 | 58 |
SHANDONG ZHI SHANG CHEMICAL CO.LTD | +86 18953170293 |
sales@sdzschem.com | China | 2931 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 |
linda@hubeijusheng.com | CHINA | 28180 | 58 |
Accela ChemBio Inc. | (+1)-858-699-3322 |
info@accelachem.com | United States | 19965 | 58 |
Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 |
alice@crovellbio.com | China | 8826 | 58 |
Xiamen AmoyChem Co., Ltd | +86-592-6051114 +8618959220845 |
sales@amoychem.com | China | 6387 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 |
linda@hubeijusheng.com | CHINA | 22968 | 58 |
Standardpharm Co. Ltd. | 86-714-3992388 |
overseasales1@yongstandards.com | United States | 14336 | 58 |
Stavudine 관련 검색:
티민 디하이드로초산나트륨 지도부딘
EC 1.1.1.28
ALDEHYDE DEHYDROGENASE
ZIDOVUDINE RELATED COMPOUND B (25 MG) (3'-CHLORO-3'-DEOXYTHYMIDINE)
5,5'-Bis(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6,6'-dichloro-3-hydroxy-3,3'-biindoline-2,2'-dione
6-Methyl-2-(4-methylphenyl)imidazol[1,2-a]-pyridine-3-acetic acid
DNA, SINGLE STRANDED, IMM. ON CELLULOSE, FROM CALF THYMUS*
2',3'-Dideoxythymidine
2,3'-ANHYDROTHYMIDINE
STAVUDINE-D3
STAVUDINE FOR SYSTEM SUITABILITY
5'-O-TRITYL-2',3'-DEHYDROTHYMIDINE
Stavudine
Deoxidizer
STAVUDINE SYSTEM SUITABILITY MIXTURE (20 MG)
3'-DEOXY 2',3'-DIDEHYDROTHYMIDINE-5'-DIPHOSPHATE