U 95133 

U 95133 is a non-nucleoside reverse transcriptase inhibitor. U 95133 exhibits activity against both wild-type and mutant HIV-1 reverse transcriptase. U 95133 can be used in studies related to HIV infection^[1][2].

U 95133 (compound 16) (0-100 μM) potently inhibits wild-type HIV-1 reverse transcriptase, with an IC₅₀ of 2.2 μM and an inhibition rate of 98% at a concentration of 100 μM^[1].
U 95133 potently inhibits HIV-1 replication in human peripheral blood mononuclear cells, with an ED₅₀ of <0.0001 μM^[1].
U 95133 (10 minutes) exhibits an IC₅₀ of 0.50 μM against wild-type HIV-1 reverse transcriptase, an IC₅₀ of 1.5 μM against HIV-1 reverse transcriptase ^P236L, and an IC₅₀ of 1.1 μM against HIV-1 reverse transcriptase ^Y181C[1].
U 95133 (4 days) potently inhibits the replication of wild-type HIV-1_IIIB in MT4 cells with an IC₉₀ of 0.02 μM, and exhibits submicromolar activity against a variety of NNRTI-resistant HIV-1 variants^[2].

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

U 95133 (15 mg/kg; i.v.; p.o.) exhibits high intravenous clearance and low oral bioavailability in rats^[1].

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

498.64

C₂₅H₃₄N₆O₃S

177577-59-2

O=C(N1CCC(CC1)N(C)C2=NC=CC=C2NC(C)(C)C)C3=CC4=C(N3)C=CC(NS(=O)(C)=O)=C4

Room temperature in continental US; may vary elsewhere.

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

• [1]. Genin MJ, et al. Synthesis and bioactivity of novel bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships and increased metabolic stability of novel substituted pyridine analogs. J Med Chem. 1996;39(26):5267-5275.

  [2]. Olmsted R A, et al. (Alkylamino) piperidine bis (heteroaryl) piperizine analogs are potent, broad-spectrum nonnucleoside reverse transcriptase inhibitors of drug-resistant isolates of human immunodeficiency virus type 1 (HIV-1) and select for drug-resistant variants of HIV-1IIIB with reduced replication phenotypes. Journal of virology, 1996, 70(6): 3698-3705.