Saquinavir mesylate
Saquinavir mesylate structure
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Common Name | Saquinavir mesylate | ||
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| CAS Number | 149845-06-7 | Molecular Weight | 766.946 | |
| Density | N/A | Boiling Point | 1015ºC at 760 mmHg | |
| Molecular Formula | C39H54N6O8S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 567.7ºC | |
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Intranasal in situ gel loaded with saquinavir mesylate nanosized microemulsion: preparation, characterization, and in vivo evaluation.
Int. J. Pharm. 475(1-2) , 191-7, (2014) Saquinavir mesylate (SM) is a protease inhibitor with activity against human immunodeficiency virus type 1 (HIV-1) and is available in tablet form, which has three major problems. First, the drug undergoes extensive first pass metabolism. Second, the drug has... |
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Saquinavir-NO-targeted S6 protein mediates sensitivity of androgen-dependent prostate cancer cells to TRAIL.
Cell Cycle 11(6) , 1174-82, (2012) We previously reported that the NO-modified form of HIV protease inhibitor Saquinavir (Saq) is a potent antitumoral agent efficient against numerous tumor cell lines in vitro and in vivo. In acute toxicity studies, doses of Saq-NO equivalent to DL100 of the p... |
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Can inhibition of proteasomes or NF-kappaB help control idiopathic nephrotic syndrome?
Nephrol. Dial. Transplant. 27(5) , 1698-701, (2012)
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Saquinavir-NO inhibits S6 kinase activity, impairs secretion of the encephalytogenic cytokines interleukin-17 and interferon-gamma and ameliorates experimental autoimmune encephalomyelitis.
J. Neuroimmunol. 259(1-2) , 55-65, (2013) NO-hybridization of the HIV protease inhibitor Saquinavir generates a new chemical entity named Saq-NO, that retains the anti-viral activity and exerts lower toxicity. We show that Saq-NO inhibited the generation of various cytokines in ConA-stimulated unfrac... |
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Stereoselective evasion of P-glycoprotein, cytochrome P450 3A, and hydrolases by peptide prodrug modification of saquinavir.
J. Pharm. Sci. 101(9) , 3199-213, (2012) In an approach to overcome biological barriers mediated by P-glycoprotein (P-gp) and cytochrome P450 3A (CYP3A), a series of stereoisomeric valine-valine prodrugs of saquinavir (SQV) were synthesized and investigated with respect to affinity for efflux pump P... |
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Impact of antiretroviral pressure on selection of primary human immunodeficiency virus type 1 envelope sequences in vitro.
J. Gen. Virol. 94(Pt 5) , 933-43, (2013) The initiation of drug therapy results in a reduction in the human immunodeficiency virus type 1 (HIV-1) population, which represents a potential genetic bottleneck. The effect of this drug-induced genetic bottleneck on the population dynamics of the envelope... |
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Perspectives on addressing ionization matrix effects in LC-MS bioanalysis.
Bioanalysis 4(10) , 1227-34, (2012) Ionization matrix effects are one of the most difficult issues in LC-MS bioanalysis that are without a good and universal solution. Most people in the field are aware of it, but some are not sure how to deal with it. Many laboratories do not routinely assess ... |
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Unique antineoplastic profile of Saquinavir-NO, a novel NO-derivative of the protease inhibitor Saquinavir, on the in vitro and in vivo tumor formation of A375 human melanoma cells.
Oncol. Rep. 28(2) , 682-8, (2012) We have recently shown that covalent attachment of the nitric oxide (NO) moiety to the HIV protease inhibitor Saquinavir (Saq) produced a qualitatively new chemical entity, named Saquinavir-NO (Saq-NO), with enhanced anticancer properties and reduced toxicity... |
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Suppression of pre adipocyte differentiation and promotion of adipocyte death by anti-HIV drugs.
In Vivo 26(2) , 287-91, (2012) In the present study, we investigated the ability of anti-HIV drugs to interfere with normal cell cycle progression and to induce oxidative stress by perturbing the redox environment. Our results provide evidence that anti-HIV drugs have a differential effect... |
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Viral protease inhibitors affect the production of virulence factors in Cryptococcus neoformans.
Can. J. Microbiol. 58(7) , 932-6, (2012) The effects of the protease inhibitors saquinavir, darunavir, ritonavir, and indinavir on growth inhibition, protease and phospholipase activities, as well as capsule thickness of Cryptococcus neoformans were investigated. Viral protease inhibitors did not re... |