1. Anti-infection
  2. Bacterial
  3. DprE1-IN-15

DprE1-IN-15 is a covalent Mycobacterium tuberculosis essential cell wall enzyme DprE1 inhibitor with an IC50 of 0.073 μM. DprE1-IN-15 forms an irreversible covalent adduct with its target enzyme. DprE1-IN-15 shows inhibitory effects against multiple Mycobacterium tuberculosis.

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DprE1-IN-15

DprE1-IN-15 Chemical Structure

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Description

DprE1-IN-15 is a covalent Mycobacterium tuberculosis essential cell wall enzyme DprE1 inhibitor with an IC50 of 0.073 μM. DprE1-IN-15 forms an irreversible covalent adduct with its target enzyme. DprE1-IN-15 shows inhibitory effects against multiple Mycobacterium tuberculosis[1].

In Vitro

DprE1-IN-15 (Compound 11c) (30 min) potently inhibits purified Mycobacterium tuberculosis DprE1 with an IC50 of 0.073 μM via covalent adduct formation[1].
DprE1-IN-15 (7 days) potently inhibits growth of drug-sensitive Mycobacterium tuberculosis H37Rv and extensively drug-resistant TB strains 13946 and 14862, with an MIC of <0.002 μM for all tested strains[1].
DprE1-IN-15 (0.26-64 μg/mL; 48 h) exhibits no significant cytotoxicity against Vero or HepG2 cells, with an IC50 of >100 μM for both cell lines[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: Vero, HepG2 cells
Concentration: 0.26-64 μg/mL
Incubation Time: 48 h
Result: Showed low cytotoxicity, with an IC50 of >100 μM against both Vero and HepG2 cells.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t F
Mice[1] 50 mg/kg p.o. 4.77 h 2.00 h 709 ng/mL 3233 ng·h/mL 31.9 %
Mice[1] 5 mg/kg i.v. 1.30 h 0.08 h 1593 ng/mL 1008 ng·h/mL /
In Vivo

DprE1-IN-15 (Compound 11c) (5-50 mg/kg; p.o., i.v.; single dose) exhibits an oral bioavailability of 31.9% in male CD-1 mice, with favorable systemic exposure following both oral and intravenous administration[1].

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

Molecular Weight

539.36

Formula

C20H21F5N4O3Se

SMILES

O=C1N=C(N2CCN(CC3CCC(F)(F)CC3)CC2)[Se]C4=C([N+]([O-])=O)C=C(C(F)(F)F)C=C14

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DprE1-IN-15
Cat. No.:
HY-183542
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