Droxinavir hydrochloride  (Synonyms: SC-55389A)

Droxinavir hydrochloride (SC-55389A) is an HIV-1 protease inhibitor. Droxinavir hydrochloride 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 hydrochloride can be used in studies related to human immunodeficiency virus type 1 infection^[1].

Droxinavir hydrochloride (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 hydrochloride (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 hydrochloride 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 hydrochloride 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.

570.21

C₂₉H₅₂ClN₅O₄

155662-50-3

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.Cl

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]