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Saquinavir mesylate
Cat No.
CEI-1517
Product Overview
Saquinavir is a potent inhibitor HIV protease with Ki value of 0.12 and <0.1 nM for HIV-1 and HIV-2 protease. HIV protease is essential for release of mature viral and viral replication which is a retroviral aspartyl protease. HIV protease cleaves the synthesized polypeptide at the appropriate places which creates the mature protein components of HIV viral. HIV-1 protease is an attractive target of AIDS. Saquinavir is a transition-state inhibitor which binds to the active site of HIV protease, preventing cleavage of viral polyproteins. Saquinavir inhibited the cleavage of p55 (the HIV-1 gag polyprotein) to p24 which is the viral structural protein in chronically infected CEM cells. The bioavailability of 20 mg/kg saquinavir increased 325-fold in mice when co-administered ritonavir at the dose of 50 mg/kg. Ritonavir prevents saquinavir from metabolizing to an inactive form by CYP3A. Saquinavir also inhibited the level of endogenous Aβ 40 from primary cultured human cortical neurons. Saquinavir significantly reduced the production of the TCA-soluble extracellular fraction at 50 or 100 μM. Saquinavir reduced Aβ production in human neurons reaching 90% at 50 μM. Saquinavir showed as high as 60, 30, 32, and 48% inhibition of BACE1 activity at 300 μM as compared to control.
CAS No.
149845-06-7
Molecular Weight
766.95
Purity
0.9906
Storage
Store at -20°C
Synonyms
Invirase; Ro 31-8959/003
Targets
HIV Protease
Molecular Formula
C39H54N6O8S
Chemical Name
(2S)-N-[(2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-(quinoline-2-carbonylamino)butanediamide; methanesulfonic acid
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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