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Saquinavir

产品号 DB01232 公司名称 DrugBank
CAS号 127779-20-8 公司网站 http://www.ualberta.ca/
分子式 C38H50N6O5 电 话 (780) 492-3111
分子量 670.8408 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 1101

产品价格信息

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产品别名

标题
Saquinavir
IUPAC标准名
(2S)-N-[(2S,3R)-4-[(3S)-3-(tert-butylcarbamoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinolin-2-ylformamido)butanediamide
IUPAC传统名
saquinavir
商标名
Fortovase
Invirase
ROC
别名
SQV
Saquinavir Mesylate
saquinavir

产品登记号

PubChem CID 60787
CAS号 127779-20-8
PubChem SID 46508726

产品性质

疏水性(logP) 3.8
溶解度 Insoluble

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved; investigational
Description An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases. [PubChem]
Indication For the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues.
Pharmacology Saquinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Saquinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
Toxicity Probably experience pain in the throat
Affected Organisms
Human Immunodeficiency Virus
Biotransformation Hepatic
Absorption Absolute bioavailability averages 4%
Protein Binding 98%
Elimination In vitro studies using human liver microsomes have shown that the metabolism of saquinavir is cytochrome P450 mediated with the specific isoenzyme, CYP3A4, responsible for more than 90% of the hepatic metabolism. Only 1% of saquinavir is excreted in the urine, so the impact of renal impairment on saquinavir elimination should be minimal.
Distribution * 700 L
Clearance * 1.14 L/h/kg [Healthy volunteers receiving IV doses of 6, 36, and 72 mg]
References
Forestier F, de Renty P, Peytavin G, Dohin E, Farinotti R, Mandelbrot L: Maternal-fetal transfer of saquinavir studied in the ex vivo placental perfusion model. Am J Obstet Gynecol. 2001 Jul;185(1):178-81. [Pubmed]
External Links
Wikipedia
RxList
Drugs.com

参考文献

  • Forestier F, de Renty P, Peytavin G, Dohin E, Farinotti R, Mandelbrot L: Maternal-fetal transfer of saquinavir studied in the ex vivo placental perfusion model. Am J Obstet Gynecol. 2001 Jul;185(1):178-81. Pubmed