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

DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.

For research use only. We do not sell to patients.

DprE1-IN-1 Chemical Structure

DprE1-IN-1 Chemical Structure

CAS No. : 920459-41-2

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Description

DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.

IC50 & Target

MICs: <0.1 μg/mL (Tuberculosis strains)[1]

In Vitro

DprE1-IN-1 (compound 17b) (64 to 0.26 μg/mL; 48 hours) has high safety with low cytotoxicity towards HepG2, J774A.1 macrophage cells (IC50>60 μg/mL) and Vero (IC50=58.18 μg/mL) alongside potent efficacy and good druggability[1].
DprE1-IN-1 can reduce 1.19 and 1.29 log10 CFU M. tuberculosis in J774A.1 macrophages at 5 μg/mL and 10 μg/mL, respectively, for 3 days treatment[1].
DprE1-IN-1 (compound 17b) (1 μM; 0-120 minutes) has high stability in human and mice hepatocytes (remaining of 42% and 49.7%, respectively; t1/2 of 24.0 and 29.7 min, respectively)[1].

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

Cell Cytotoxicity Assay

Cell Line: Vero, HepG2 and mouse J774A.1 macrophage cells[1]
Concentration: 64 to 0.26 μg/mL
Incubation Time: 48 hours
Result: Displayed high safety with low cytotoxicity towards HepG2, J774A.1 macrophage cells (IC50>60 μg/mL) and Vero (IC50=58.18 μg/mL) alongside potent efficacy and good druggability.
In Vivo

DprE1-IN-1 (100 mg/kg; oral gavage; 5 days per week from day 10 until day 30) can reduce the bacterial burden in the lungs by 0.54 log10 CFU after three weeks of treatment in M. tuberculosis H37Rv infected mice[1].

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

Animal Model: Female SPF Balb/c mice (18-20 g) (M. tuberculosis H37Rv infected)[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 5 days per week from day 10 until day 30
Result: Reduced the bacterial burden in the lungs by 0.54 log10 CFU compared with the untreated control group after three weeks of treatment.
Molecular Weight

451.52

Formula

C19H21N3O6S2

CAS No.
SMILES

O=C(OCC)NC(C1=C(NC(C2=CC=C(S(=O)(N3CCCC3)=O)C=C2)=O)SC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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DprE1-IN-1 Related Classifications

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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-1
Cat. No.:
HY-144341
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