Droxinavir  (Synonyms: SC-55389A free base)

Droxinavir (SC-55389A free base) is an HIV-1 protease inhibitor. Droxinavir binds to the S2 and S2' subsites of HIV-1 protease, and this interaction is regulated by protease amino acid residue 88, where the N88S mutation confers viral resistance. Droxinavir can be used in studies related to human immunodeficiency virus type 1 infection^[1].

Droxinavir (1 μM; 9 weekly passages) selects for resistant HIV-1 89-959 variants with the N88S protease mutation, which retain resistance to the compound for 9 weekly passages and exhibit an EC₅₀ of 580 nM; resistance persists after 26 passages without drug, with an EC₅₀ of 734 nM, and additional selection yields a variant with an EC₅₀ of 901 nM^[1].
Droxinavir (50 nM-16 μM; 21 weekly passages) selects for resistant HIV-1 LAI variants with L10F and N88S protease mutations, and these variants exhibit an EC₅₀ of 901 nM^[1].
Droxinavir has reduced efficacy against HIV-1 HXB2 clones with the N88S protease mutation alone or combined with L10F in MT2 cells, with EC₅₀ values of 46 nM and 61 nM, respectively^[1].
Droxinavir potently inhibits wild-type HIV-1 SF162 in PBMCs with an EC₅₀ of 11 nM, and SC-52151-selected HIV-1 SF162 variants retain susceptibility to the compound with an EC₅₀ of 4.0 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

533.75

C₂₉H₅₁N₅O₄

159910-86-8

O[C@H](CN(C(NC(C)(C)C)=O)CCC(C)C)[C@@H](NC([C@H](C(C)(C)C)NC(CNC)=O)=O)CC1=CC=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Smidt ML, et al. A mutation in human immunodeficiency virus type 1 protease at position 88, located outside the active site, confers resistance to the hydroxyethylurea inhibitor SC-55389A. Antimicrob Agents Chemother. 1997;41(3):515-522.  [Content Brief]