라미부딘
|
|
라미부딘 속성
- 녹는점
- 177 °C
- 알파
- D21 -135° (c = 0.38 in methanol)
- 끓는 점
- 475.4±55.0 °C(Predicted)
- 밀도
- 1.73±0.1 g/cm3(Predicted)
- 굴절률
- -142 ° (C=1, MeOH)
- 인화점
- 9℃
- 저장 조건
- 2-8°C
- 용해도
- 물: 용해성10mg/mL, 투명
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 13.83±0.10(Predicted)
- 색상
- 흰색에서 베이지색
- 수용성
- 70g/L(온도 미표시)
- Merck
- 14,5352
- BCS Class
- 1,3
- 안정성
- 제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 -20°C에서 최대 1개월 동안 보관할 수 있습니다.
- InChIKey
- JTEGQNOMFQHVDC-NKWVEPMBSA-N
- CAS 데이터베이스
- 134678-17-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험 카페고리 넘버 | 63-36/37/38 | ||
---|---|---|---|
안전지침서 | 26-36 | ||
유엔번호(UN No.) | UN1230 - class 3 - PG 2 - Methanol, solution | ||
WGK 독일 | 3 | ||
RTECS 번호 | UW7361333 | ||
HS 번호 | 29349990 | ||
유해 물질 데이터 | 134678-17-4(Hazardous Substances Data) |
라미부딘 C화학적 특성, 용도, 생산
개요
라미부딘 (Lamivudine)은 역전사 효소 억제제이며, 황 원자가 5 탄당 고리의 3 '탄소를 대체하는 잘시 타빈 유사체이다.용도
그것은 인간 면역 결핍 바이러스를 예방하고 치료할 수있는 항 바이러스 활성 성분입니다. 라미부딘은 우리 몸에 B 형 간염 바이러스가 번식하는 것을 막을 때도 효과적입니다. 라미부딘은 경구 투여 후에 매우 빠르게 흡수됩니다.개요
Lamivudine is a new generation orally active nucleoside analog launched in the U.S.A. for use in combination with zidovudine (AZT) as a first-line therapy for patients with HIV infection. Lamivudine is rapidly converted to phosphorylated metabolites in the body which act as inhibitors and chain terminators of HIV reverse transcriptase (RT), the enzyme required for the replication of the HIV genome. Lamivudine has similar inhibitory potency to RT as AZT but is 10 times less toxic and is active against AZT-resistant strains of HIV.화학적 성질
White solid from methanol-ethyl acetate. [α]D21-132° (C=1.08, methanol). Or crystallised from boiling ethanol, melting point 160-162°C. [α]D21-135° (C=0.38, methanol).역사
Lamivudine[134678-17-4] is produced by GlaxoSmithKline LLC. In the early 1990s, it was used by some countries in Europe and North America to treat AIDS. In the mid-1990s, medical experts found that it had an inhibitory effect on the DNA of hepatitis B virus. In 1998, the US Food and Drug Administration (FDA) first approved it as a treatment drug for hepatitis B. In 1999, the China Food and Drug Administration approved this drug as a hepatitis B treatment drug, with the Chinese trade name "Heputin".용도
Lamivudine (Epivir-HBV) is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HIV and hepatitis B in the blood. It is used to treat hepatitis B infection. It is also used along with other medications to treat human immunodeficiency virus (HIV) infection in adults and children 3 months of age and older.정의
ChEBI: Lamivudine is a monothioacetal that consists of cytosine having a (2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl moiety attached at position 1. An inhibitor of HIV-1 reverse transcriptase.Synthesis
Aqueous hydrochloric acid (6N, 30 ml) was slowly added to a solution of 20 gm of the solid (2R-cis)-4-Amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidi- none.S-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate in water (200 ml) at 45-50 deg C. Stirred the reaction for 1 hour at room temperature. The solid S-1,1'-binaphthyl-2,2'-diyl hydrogen phosphate was filtered and the aqueous layer was neutralized with aqueous sodium hydroxide solution (30%, 20 ml). The solvent was recovered under vacuum at 40-45 deg C., the product obtained was dissolved in methanol (200 ml), filtered to remove the inorganic salts, the filtrate was concentrated under vacuum at 40-45 deg C. and the residual solid obtained was dissolved in ethanol (50 ml), heated to 50 deg C., slowly allowed to room temperature, cooled to 10 deg C., filtered and dried at 40-45 deg C. to obtain 5 gm of Lamivudine(Chiral purity: 97.5%).![synthesis of Lamivudine](/NewsImg/2022-09-27/6379986649824383064894319.jpg)
원료
Long-term lamivudine administration frequently elicits viral resistance characterized by a reincrease of viral replication in an adherent patient. The incidence of lamivudine resistance is 14% to 32% after 1 year of treatment, 38% after 2 years, and 53% to 76% after 3 years.Pharmacokinetics
The pharmacokinetics of lamivudine are similar in patients with HIV-1 or HBV infection, and healthy volunteers. The drug is rapidly absorbed after oral administration, with maximum serum concentrations usually attained 0.5 to 1.5 hours after the dose.Clinical Use
Lamivudine is indicated for the treatment of HIV when used in combination with other antiretroviral agents.A lower dose than that used to treat HIV is approved for the treatment of HBV.부작용
Lamivudine oral tablet can cause mild or serious side effects. The more common side effects that can occur with lamivudine include:cough,diarrhea,fatigue,headache,malaise (general discomfort),nasal symptoms, such as a runny nose,nausea.
참고 문헌
[1] ROUSSOSA. Lamivudine treatment for acute severe hepatitis B: report of a case and review of the literature.[J]. Acta gastro-enterologica Belgica, 2008, 71 1: 30-32.[2] ARTSE J WainbergM A. Mechanisms of nucleoside analog antiviral activity and resistance during human immunodeficiency virus reverse transcription.[J]. Antimicrobial Agents and Chemotherapy, 1996, 40 3: 527-540. DOI:10.1128/AAC.40.3.527.
[3] COATESJ A. (-)-2’-deoxy-3’-thiacytidine is a potent, highly selective inhibitor of human immunodeficiency virus type 1 and type 2 replication in vitro.[J]. Antimicrobial Agents and Chemotherapy, 1992, 36 4: 733-739. DOI:10.1128/AAC.36.4.733.
[4] KONGHUI. Targeted P2X7/NLRP3 signaling pathway against inflammation, apoptosis, and pyroptosis of retinal endothelial cells in diabetic retinopathy.[J]. Cell Death & Disease, 2022, 13 4: 336. DOI:10.1038/s41419-022-04786-w.
[5] KUMAR P N, PATEL P. Lamivudine for the treatment of HIV[J]. Expert Opinion on Drug Metabolism & Toxicology, 2010, 6: 105-114. DOI:10.1517/17425250903490418.
[6] PERRYC M FauldsD. Lamivudine. A review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in the management of HIV infection.[J]. Drugs, 1997, 53 4: 657-680. DOI:10.2165/00003495-199753040-00008.
[7] RAJURKARMIHIR. Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer.[J]. Cancer discovery, 2022, 12 6: 1462-1481. DOI:10.1158/2159-8290.CD-21-1117.
라미부딘 준비 용품 및 원자재
원자재
실리카겔
납 테트라아세트산
실란
염화에틸
나트륨 붕소수화물
나트륨 과요오드산
Bromide
테트라뷰틸암모늄 플루오린화물
Praseodymium(III) nitrate hexahydrate
헥사메틸다이실라잔
브로모아세트알데히드디에틸아세탈
트리메틸클로로실란
시토신
티오안식향산
P-톨루엔설폰 산
포타슘터셔리부톡사이드
준비 용품
라미부딘 공급 업체
글로벌( 746)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Coben pharmaceutical Co., Ltd | |
13456759982@126.com | United States | 1 | 58 |
Hebei Guanlang Biotechnology Co,.LTD | +8619930503252 |
daisy@crovellbio.com | China | 5828 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 |
xie@china-sinoway.com | China | 990 | 58 |
Sigma Audley | +86-18336680971 +86-18126314766 |
nova@sh-teruiop.com | China | 491 | 58 |
Shaanxi TNJONE Pharmaceutical Co., Ltd | +8618740459177 |
sarah@tnjone.com | China | 1143 | 58 |
Hebei Ganmiao New material Technology Co., LTD | +86-17332992504 +86-17332992504 |
sales8@hbganmiao.com | China | 300 | 58 |
Frapp's ChemicalNFTZ Co., Ltd. | +86 (576) 8169-6106 |
sales@frappschem.com | China | 885 | 50 |
Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21668 | 55 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9332 | 55 |
라미부딘 관련 검색:
트리스(하이드록시메틸)아미노메탄 1.4-다이옥세인 글리신 6-아미노 카프로산 트리스(하이드록시메틸)니트로메탄 지도부딘 시토신 라미부딘
ALTRENOGEST
Adefovir dipivoxil
Entecavir
(1R,2S,5R)-Menthyl-(2R,5S)-5-(4-amino-2-oxo-2H-pyrimidin-1-yl)-[1,3]oxathiolane-2-carboxylic acid
Lamivudine Resolution Mixture B
Lamivudine salicylate
Emtricitabine
[1R-[1(2S*,5R*),2beta,5alpha]]-5-(4-Amino-5-fluoro-2-oxo-1(2H)-pyrimidinyl)-1,3-oxathiolane-2-carboxylic acid 5-methyl-2-(1-methylethyl)cyclohexyl ester
LAMIVUDINE FOR SYSTEM SUITABILITY 1
LAMIVUDINE-15N2,13C