Prezista Inhibitor CAS No. 635728-49-3

Cat. No.	Name	Size	Price	Add Cart
KI0687	Prezista	5 mg	$550
KI0687	Prezista	50 mg	$2200

Chemical Characteristic

Product Name	Prezista
Synonyms	Darunavir ethanolate,TMC114,UIC-94017
CAS No.	635728-49-3
Molecular Weight	593.73
Formula	C₂₇H₃₇N₃O₇S.C₂H₆O
Chemical Structure

Biological activities

Prezista is the ethanolate salt of darunavir. Darunavir is a HIV-1 protease inhibitor.^[1]Darunavir is a second-generation protease inhibitor. Darunavir has P-gp inhibitory property.^[2] Darunavir inhibits HIV-1 LA1 and HIV-1 SF2 in peripheral blood mononuclear cells with IC50 of 1 and 1.6 nM, respectively.^[3] Darunavir blocks the infectivity and replication of each of HIV-1_{NL4-3 variants. Darunavir has potent activity against HIV-1_{BaL with an IC50 of 3 nM. ^[4] Darunavir has an IC50 of ~5 nM to inhibit the production of p24.^[4]}}

Protocols

In vitro: TMC114 is dissolved in DMSO.^[1]

References

[1] Kovalevsky AY, et al. Ultra-high resolution crystal structure of HIV-1 protease mutant reveals two binding sites for clinical inhibitor TMC114. J Mol Biol. 2006, 363(1): 161-173. [2] Holmstock N, et al. In situ intestinal perfusion in knockout mice demonstrates inhibition of intestinal p-glycoprotein by ritonavir causing increased darunavir absorption. Drug Metab Dispos. 2010, 38(9): 1407-1410. 閵嗏偓閵嗏偓 [3] Yilmaz A, et al. TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob Agents Chemother. 2005, 49(6): 2314-2321. [4] Koh Y, et al. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob Agents Chemother. 2003, 47(10): 3123-3129. 閵嗏偓閵嗏偓 [5] Huang L, et al. Flexible catalytic site conformations implicated in modulation of HIV-1 protease autoprocessing reactions. Retrovirology. 2011, 8: 79. 閵嗏偓閵嗏偓

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