NBD-11021

NBD-11021 is a HIV-1 entry antagonist and CD4 antagonist. NBD-11021 binds to the Phe43 cavity of HIV-1 gp120 and competitively blocks the gp120-CD4 interaction. NBD-11021 exhibits broad-spectrum inhibitory activity against 56 HIV-1 Env pseudoviruses of different subtypes, with an IC₅₀ of 0.6-5.3 μM. NBD-11021 inhibits CCR5- and CXCR4-tropic HIV-1, primary HIV-1, drug-resistant HIV-1, HIV-1 Env-mediated cell fusion and intercellular viral transmission. NBD-11021 can be used in studies related to HIV-1 gp120, viral entry and HIV infection^[1][2][3][4]. In Vitro:NBD-11021 (compound 89) inhibits CCR5-tropic HIV-1_ADA and CXCR4-tropic HIV-1_HXB2 infection in U87-CD4-CCR5 and U87-CD4-CXCR4 cells, respectively, with IC₅₀ values of 1.7 μM and 2.4 μM^[3].
NBD-11021 exhibits broad-spectrum inhibitory activity against 56 HIV-1 Env pseudoviruses covering multiple clades, with an IC₅₀ range of 0.6-5.3 μM and a mean IC₅₀ of 2.38 μM^[3].
NBD-11021 inhibits cell-to-cell transmission of CXCR4-tropic and CCR5-tropic HIV-1 in a co-culture system of GHOST X4/R5 target cells and chronically infected effector cells^[3].
NBD-11021 inhibits single-cycle infection of HIV-1_HXB2 in TZM-bl cells and multi-cycle infection of HIV-1_IIIB in MT-2 cells, with IC₅₀ values of 2.2 μM and 0.85 μM, respectively^[1].
NBD-11021 (pretreated for 1 h followed by 24 h of co-culture) inhibits HIV-1 Env-mediated cell fusion between MAGI-CCR5 and HL2/3 cells, with an IC₅₀ of 6.1 μM^[1].
NBD-11021 inhibits laboratory-adapted, primary, and drug-resistant HIV-1 strains, including AZT-resistant strains, protease inhibitor-resistant strains, and gp41 fusion inhibitor-resistant strains, in MT-2 cells or PBMC^[3].
NBD-11021 (pretreated for 1 h; co-cultured for 24 h) inhibits HIV-1 Env-mediated cell fusion between MAGI-CCR5 and HL2/3 cells, with an IC₅₀ of 9.8 μM^[3].