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Darunavir HIV-1 protease inhibitor

Catalog No.A8206
Size Price Stock Qty
10mM (in 1mL DMSO)
$140.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$60.00
In stock
50mg
$330.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Lan, Jie, et al. "Provirus Activation Plus CD59 Blockage Triggers Antibody-Dependent Complement-Mediated Lysis of Latently HIV-1–Infected Cells." The Journal of Immunology (2014): 1303030. PMID:25149467

Biological Activity

Description Darunavir is an inhibitor of HIV protease.
Targets HIV Protease          
IC50            

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Chemical Properties

Cas No. 206361-99-1 SDF Download SDF
Chemical Name (E)-(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl hydrogen ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbonimidate
Canonical SMILES CC(CN(S(C1=CC=C(N)C=C1)(=O)=O)C[[email protected]](O)([H])[[email protected]](/N=C(O[[email protected]@]2([H])CO[[email protected]]3([H])[[email protected]@]2([H])CCO3)\O)([H])CC4=CC=CC=C4)C
Formula C27H37N3O7S M.Wt 547.66
Solubility >22.7mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Darunavir is an orally-bioavailable non-peptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that selectively inhibits HIV-1 protease enzyme induced cleavage of gag and gag-pol poly-proteins preventing the maturation of virions and also inhibits the dimerization of HIV-1 protease suppressing proteolytic activity and subsequent replication of HIV-1. Study results have shown that darunavir exhibits potent inhibition against HIV-1 with a value of 50% inhibition concentration IC50 of 0.003 μmol/L in HIV-1 infected MT-2 cells. Darunavir binds to HIV-1 protease with considerably high affinity and fits closely with the substrate envelop leading to its potent ability to inhibit multidrug-resistant HIV strains.

Reference

McKeage K, Perry CM, Keam SJ. Darunavir: a review of its use in the management of HIV infection in adults. Drugs. 2009;69(4):477-503. doi: 10.2165/00003495-200969040-00007.