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Darunavir Ethanolate

Catalog No.
B4950
nonpeptidic HIV protease inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
5mg
$60.00
In stock
50mg
$330.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Darunavir ethanolate is a nonpeptidic HIV protease inhibitor approved for the treatment of HIV infection[1]. 

Transepithelial transport of darunavir in Caco-2 cell monolayers is 2-fold greater in the basal-to-apical direction compared to that in the opposite direction. In L-MDR1 cell, darunavir (121 mM) inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester[1]. 

Darunavir is effective against wild-type and PI-resistant HIV, and has a low oral bioavailability (37%). When used in combination with ritonavir, bioavailability can be increased to 82%[2]. 

References:

[1]. Fujimoto H, Higuchi M, Watanabe H, et al. P-Glycoprotein Mediates Efflux Transport of Darunavir in Human Intestinal Caco-2 and ABCB1 Gene-Transfected Renal LLC-PK1 Cell Lines. Biological & Pharmaceutical Bulletin, 2009, 32(9): 1588-1593.

[2]. Bhalekar MR, et al. In-vivo bioavailability and lymphatic uptake evaluation of lipid nanoparticulates of darunavir. Drug Deliv, 2016, 23(7): 2581-2586.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt593.73
Cas No.635728-49-3
FormulaC29H43N3O8S
Solubility≥21 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate compound with ethanol (1:1)
SDFDownload SDF
Canonical SMILESO[[email protected]](CN(CC(C)C)S(=O)(C(C=C1)=CC=C1N)=O)[[email protected]](CC2=CC=CC=C2)NC(O[[email protected]@H]3[[email protected]]4[[email protected]](OCC4)OC3)=O.OCC
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control