NBD-09027
NBD-09027 is a HIV-1 gp120 inhibitor. NBD-09027 blocks the gp120-CD4 interaction by binding to the Phe43 cavity of gp120, thereby inhibiting HIV-1-mediated cell fusion and the infectivity of multiple viral subtypes. NBD-09027 can be used in studies of human immunodeficiency virus type 1 infection.
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- CAS No.: 1376434-43-3
- Formule: C19H23ClN4O3S
- Masse moléculaire:422.93
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
HIV |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H9 | IC50 |
2.3 μM
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Inhibition of cell-cell fusion between HIV-1(IIIB)-infected H9 human T-cell leukemia cells and MT-2 human T-cell leukemia cells assessed by counting fused and unfused calcein-labeled cells after 3 h incubation by inverted fluorescence microscope.
Inhibition of cell-cell fusion between HIV-1(IIIB)-infected H9 human T-cell leukemia cells and MT-2 human T-cell leukemia cells assessed by counting fused and unfused calcein-labeled cells after 3 h incubation by inverted fluorescence microscope.
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25001301 |
| TZM | IC50 |
0.7 μM
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Inhibition of infection by clade C ZM135M.PL10a HIV-1 Env-pseudotyped reference virus in TZM-bl cells assessed by luciferase activity after 3 days incubation following 30 min preincubation of virus with reagent.
Inhibition of infection by clade C ZM135M.PL10a HIV-1 Env-pseudotyped reference virus in TZM-bl cells assessed by luciferase activity after 3 days incubation following 30 min preincubation of virus with reagent.
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25001301 |
| TZM | IC50 |
> 21 μM
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Inhibition of infection by clade C ZM197M.PB7 and ZM214M.PL15 HIV-1 Env-pseudotyped reference viruses in TZM-bl cells assessed by luciferase activity after 3 days incubation following 30 min preincubation of virus with reagent.
Inhibition of infection by clade C ZM197M.PB7 and ZM214M.PL15 HIV-1 Env-pseudotyped reference viruses in TZM-bl cells assessed by luciferase activity after 3 days incubation following 30 min preincubation of virus with reagent.
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25001301 |
| TZM | CC50 |
> 32 μM
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Cytotoxicity against TZM-bl cells.
Cytotoxicity against TZM-bl cells.
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25001301 |
| MT2 | IC50 |
4 μM
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Inhibition of laboratory-adapted HIV-1 isolates in human MT-2 cells assessed via p24 antigen ELISA after 4 days of incubation during viral infection.
Inhibition of laboratory-adapted HIV-1 isolates in human MT-2 cells assessed via p24 antigen ELISA after 4 days of incubation during viral infection.
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25001301 |
| MT2 | IC50 |
35.8 μM
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Inhibition of laboratory-adapted HIV-1 isolates in human MT-2 cells assessed via p24 antigen ELISA after 4 days of incubation during viral infection.
Inhibition of laboratory-adapted HIV-1 isolates in human MT-2 cells assessed via p24 antigen ELISA after 4 days of incubation during viral infection.
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25001301 |
In Vitro
NBD-09027 (3 h) inhibits HIV-1-mediated cell-cell fusion between HIV-1IIIB-infected H9 cells and MT-2 cells, with an IC50 of 2.3 μM[1].
NBD-09027 (1 h) blocks the binding of CD4 to recombinant HIV-1IIIB gp120, with an IC50 of 6.2 μM[1].
NBD-09027 inhibits the infection of U87-CD4-CCR5 cells by R5-tropic NL4-3-ADA-Luc pseudovirus (IC50 = 9.1 μM) and the infection of U87-CD4-CXCR4 cells by X4-tropic NL4-3-HXB2-Luc pseudovirus (IC50 = 8.6 μM)[1].
NBD-09027 potently and selectively inhibits the infection of TZM-bl cells by multiple HIV-1 Env pseudotyped reference viruses of subtypes A, A/D, A2/D, A/E, A/G, B, C, and D, with IC50 values ranging from 0.7 μM to > 21 μM and a CC50 value of > 32 μM[1].
NBD-09027 (30-55 μM; for up to 9 weeks) selects drug-resistant viruses carrying the NN301-302KI, K432R, and V782L mutations during serial passage of NL4-3 HIV-1 in Jurkat cells[1].
NBD-09027 (4-7 days) inhibits the laboratory-adapted HIV-1 isolate in MT-2 cells with an IC50 range of 4-35.8 μM, but exhibits only weak or no activity against primary HIV-1 isolates of subtype C and group O in PBMCs[2].
NBD-09027 (4 h) exhibits weak inhibitory activity against the cell-to-cell transmission of CXCR4-tropic HIV-1 in GHOST (3) X4/R5 cells, with an IC50 of approximately 60 μM, and shows no inhibitory activity against the cell-to-cell transmission of CCR5-tropic HIV-1[2].
NBD-09027 (10-50 μM) dose-dependently inhibits the infectivity of CD4-dependent HIV-1 NL4-3-ADA-Luc in CD4-positive Cf2Th-CD4-CCR5 cells, with more potent inhibitory effects at higher concentrations up to 50 μM; meanwhile, it dose-dependently enhances the infectivity of CD4-independent HIV-1 NL4-3-ADA-N197S-Luc in CD4-negative Cf2Th-CCR5 cells[1].
NBD-09027 (10-50 μM) inhibits the infectivity of ENV-pseudotyped HIV-1 strains NIH #11313, NIH #11906, NIH #11601, and NIH #11890 in a dose-dependent manner, and its inhibitory effect increases when the concentration is elevated to 50 μM[1].
NBD-09027 (compound 6) exhibits consistently enhanced anti-HIV-1 activity against the vast majority of HIV-1 subtypes represented by a panel of 53 reference Env pseudoviruses[1].
NBD-09027 significantly reduces the CD4 agonist activity. Drug resistance selection confirms that it binds to the CD4 binding site on HIV-1 gp120, and mutations are detected at concentrations of 44 μM and 55 μM [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1376434-43-3
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Masse moléculaire 422.93
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Formule C19H23ClN4O3S
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SMILES
O=C(C(NC(C1NCCCC1)C2=NC(C)=C(CO)S2)=O)NC3=CC=C(C=C3)Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Curreli F, et al. Binding mode characterization of NBD series CD4-mimetic HIV-1 entry inhibitors by X-ray structure and resistance study. Antimicrob Agents Chemother. 2014 Sep;58(9):5478-91. [Content Brief]
[3]. Curreli F, et al. Structure-Based Design of a Small Molecule CD4-Antagonist with Broad Spectrum Anti-HIV-1 Activity. Journal of medicinal chemistry. 2015 Sep 10;58(17):6909-6927. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NBD-09027 Related Classifications
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