INDINAVIR SULFATE
Synonyms. Indinavir Sulfate; (alphaR,gammaS,2S)-alpha-Benzyl-2-(tert-butylcarbamoyl)- gamma-hydroxy-N-((1S,2R)-2-hydroxy-1-indanyl)-4-(3-pyridylmethyl)-1- piperazinevaleramide sulfate; Crixivan; 2,3,5-Trideoxy-N-((1S,2R)-2,3-dihydro-2-hydroxy-1H-inden-1-yl)- 5-((2S)-2-(((1,1-dimethylethyl)amino)carbonyl)-4-( 3-pyridinylmethyl)-1-piperazinyl)-2-(phenylmethyl)-D-erythro-pentonamide sulfate

INDINAVIR
 

PRODUCT IDENTIFICATION

CAS RN

 150378-17-9 (parent), 157810-81-6 (sulfate), 180683-37-8 (hydrate)

EINECS RN

 207-586-9

FORMULA

 C36H47N5O4·H2SO4

MOLE WEIGHT

 711.87

H.S CODE

 2933.59.3600

SMILES

 c12[C@@H]([C@H](O)Cc1cccc2)NC([C@@H](Cc1ccccc1) C[C@@H](C[N@@]1[C@@H](C[N@@](Cc2cccnc2)CC1)C(NC(C)(C)C) =O)O)=O.S(O)(O)(=O)=O

CLASSIFICATION

Antiretroviral, Antiviral, Protease inhibitor,

EXTRA NOTES

 A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE.

white crystalline powder

MELTING POINT

150 - 153 C

BOILING POINT

  

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STABILITY AND REACTIVITY
STABILITY Stable under normal conditions.

INCOMPATIBLE MATERIALS

Oxidizing agents
POLYMERIZATION

Has not been reported

NFPA RATINGS

 

 

EXTERNAL LINKS & GENERAL DESCRIPTION

Wikipedia Linking

Google Scholar Search

Drug Information Portal (U.S. National Library of Medicine) - Indinavir

PubChem Compound Summary - Indinavir sulfate

Drug Bank -  Indinavir

KEGG (Kyoto Encyclopedia of Genes and Genomes) -  Indinavir

http://www.ebi.ac.uk/chebi/ -  Indinavir

http://www.ncbi.nlm.nih.gov/ - Indinavir

http://www.antimicrobe.org/
Class:Indinavir is an HIV protease inhibitor. Antiviral Activity: Indinavir has activity against HIV-1 and HIV-2. Mechanism of Action: Cleavage of polyproteins by the protease enzyme is an essential step in the HIV life cycle. After cleavage the immature virus proteins are assembled into particles which bud from the cell as mature, infectious virons. Protease inhibitors compete for the active cleavage site on the protease enzyme, blocking the cleavage of the polyproteins and thus the maturation of new viral particles. Mechanism of Resistance: Higher levels of protease inhibitor resistance result from the accumulation of multiple protease inhibitor-resistance mutations. There are multiple mechanisms of resistance. These include reduced binding affinity between the inhibitor and the protease enzyme, alterations in enzyme catalysis, effects on dimer stability, alterations in inhibitor binding kinetics and re-shaping of the active site.

http://www.medicinenet.com/
DRUG CLASS AND MECHANISM: Indinavir is an oral medication that is used for treating infections with the human immunodeficiency virus (HIV). It is in a class of drugs called protease inhibitors which also includes ritonavir (Norvir), nelfinavir (Viracept) and saquinavir (Invirase, Fortovase). During infection with HIV, the HIV virus multiplies within the body's cells. Viruses are released from the cells and spread throughout the body where they infect other cells. In this manner, HIV infection is perpetuated among new cells that the body produces continually. During the production of the viruses, new proteins are made. Some of the proteins are structural proteins, that, is, proteins that form the body of the virus. Other proteins are enzymes which manufacture DNA and other components for the new viruses. Protease is the enzyme that forms the new structural proteins and enzymes. Indinavir blocks the activity of protease and results in the formation of defective viruses that are unable to infect the body's cells. As a result, the number of viruses in the body (the viral load) decreases. Nevertheless, indinavir does not prevent the transmission of HIV among individuals, and it does not cure HIV infections or AIDS. Indinavir was approved by the FDA in March, 1995.

 

SALES SPECIFICATION

APPEARANCE

white crystalline powder

PURITY

99.0% min

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

Not regulated

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SAFETY INFORMATION

HAZARD OVERVIEW

Not known

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PRICE INFORMATION